Kevan Shokat, PhD

The structure of KRASG12C bound to divarasib highlights features of potent switch-II pocket engagement.

Small GTPases

Fernando MC, Craven GB, Shokat KM

Deazaguanylation is a nucleobase-protein conjugation required for type IV CBASS immunity.

bioRxiv : the preprint server for biology

Wassarman DR, Pfaff P, Paulo JA, Gygi SP, Shokat KM, Kranzusch PJ

HBV Remodels PP2A Complexes to Rewire Kinase Signaling in Hepatocellular Carcinoma.

Cancer research

Turnham RE, Pitea A, Jang GM, Xu Z, Lim HC, Choi AL, Von Dollen J, Levin RS, Webber JT, McCarthy E, Hu J, Li X, Che L, Singh A, Yoon A, Chan G, Kelley RK, Swaney DL, Zhang W, Bandyopadhyay S, Theis FJ, Eckhardt M, Chen X, Shokat KM, Ideker T, Krogan NJ, Gordan JD

Direct RAS inhibitors turn 10.

Nature chemical biology

Ostrem JML, Peters U, Shokat KM

Subcellular activation of β-adrenergic receptors using a spatially restricted antagonist.

Proceedings of the National Academy of Sciences of the United States of America

Liccardo F, Morstein J, Lin TY, Pampel J, Lang D, Shokat KM, Irannejad R

Targeting Ras-, Rho-, and Rab-family GTPases via a conserved cryptic pocket.

Cell

Morstein J, Bowcut V, Fernando M, Yang Y, Zhu L, Jenkins ML, Evans JT, Guiley KZ, Peacock DM, Krahnke S, Lin Z, Taran KA, Huang BJ, Stephen AG, Burke JE, Lightstone FC, Shokat KM

IL-13 and IL-17A activate ß1 integrin through an NF-kB/Rho kinase/PIP5K1? pathway to enhance force transmission in airway smooth muscle.

Proceedings of the National Academy of Sciences of the United States of America

Ngo U, Shi Y, Woodruff P, Shokat K, DeGrado W, Jo H, Sheppard D, Sundaram AB

Absence of ABL1 exon 2-encoded SH3 residues in BCR::ABL1 destabilizes the autoinhibited kinase conformation and confers resistance to asciminib.

Leukemia

Leyte-Vidal A, DeFilippis R, Outhwaite IR, Kwan I, Lee JY, Leavitt C, Miller KB, Rea D, Rangwala AM, Lou K, Patel S, Alvarez A, Shokat KM, Bahar I, Seeliger MA, Shah NP

Acute rapamycin treatment reveals novel mechanisms of behavioral, physiological, and functional dysfunction in a maternal inflammation mouse model of autism and sensory over-responsivity.

bioRxiv : the preprint server for biology

Le Belle JE, Condro M, Cepeda C, Oikonomou KD, Tessema K, Dudley L, Schoenfield J, Kawaguchi R, Geschwind D, Silva AJ, Zhang Z, Shokat K, Harris NG, Kornblum HI

IL-13 and IL-17A Activate β1 Integrin through an NF-kB/Rho kinase/PIP5K1γ pathway to Enhance Force Transmission in Airway Smooth Muscle.

bioRxiv : the preprint server for biology

Ngo U, Shi Y, Woodruff P, Shokat K, DeGrado W, Jo H, Sheppard D, Sundaram AB

Strain-release alkylation of Asp12 enables mutant selective targeting of K-Ras-G12D.

Nature chemical biology

Zheng Q, Zhang Z, Guiley KZ, Shokat KM

Nanomolar Protein Thermal Profiling with Modified Cyanine Dyes.

Analytical chemistry

Malakoutikhah M, Mahran R, Gooran N, Masoumi A, Lundell K, Liljeblad A, Guiley K, Dai S, Zheng Q, Zhu L, Shokat KM, Kopra K, Härmä H

Selective activation of intracellular β1AR using a spatially restricted antagonist.

bioRxiv : the preprint server for biology

Liccardo F, Morstein J, Lin TY, Pampel J, Shokat KM, Irannejad R

Protocol for performing and optimizing differential scanning fluorimetry experiments.

STAR protocols

Wu T, Hornsby M, Zhu L, Yu JC, Shokat KM, Gestwicki JE

Proteomic and genetic analyses of influenza A viruses identify pan-viral host targets.

Nature communications

Haas KM, McGregor MJ, Bouhaddou M, Polacco BJ, Kim EY, Nguyen TT, Newton BW, Urbanowski M, Kim H, Williams MAP, Rezelj VV, Hardy A, Fossati A, Stevenson EJ, Sukerman E, Kim T, Penugonda S, Moreno E, Braberg H, Zhou Y, Metreveli G, Harjai B, Tummino TA, Melnyk JE, Soucheray M, Batra J, Pache L, Martin-Sancho L, Carlson-Stevermer J, Jureka AS, Basler CF, Shokat KM, Shoichet BK, Shriver LP, Johnson JR, Shaw ML, Chanda SK, Roden DM, Carter TC, Kottyan LC, Chisholm RL, Pacheco JA, Smith ME, Schrodi SJ, Albrecht RA, Vignuzzi M, Zuliani-Alvarez L, Swaney DL, Eckhardt M, Wolinsky SM, White KM, Hultquist JF, Kaake RM, García-Sastre A, Krogan NJ

Direct Modulators of K-Ras-Membrane Interactions.

ACS chemical biology

Morstein J, Shrestha R, Van QN, López CA, Arora N, Tonelli M, Liang H, Zhou Y, Hancock JF, Stephen AG, Turbyville TJ, Shokat KM

Evolutionarily divergent mTOR remodels translatome for tissue regeneration.

Nature

Zhulyn O, Rosenblatt HD, Shokat L, Dai S, Kuzuoglu-Öztürk D, Zhang Z, Ruggero D, Shokat KM, Barna M

mTOR inhibition reprograms cellular proteostasis by regulating eIF3D-mediated selective mRNA translation and promotes cell phenotype switching.

Cell reports

Shin S, Han MJ, Jedrychowski MP, Zhang Z, Shokat KM, Plas DR, Dephoure N, Yoon SO

Chemical Genetic Identification of PKC Epsilon Substrates in Mouse Brain.

Molecular & cellular proteomics : MCP

Dugan MP, Ferguson LB, Hertz NT, Chalkley RJ, Burlingame AL, Shokat KM, Parker PJ, Messing RO

A reversible SRC-relayed COX2 inflammatory program drives resistance to BRAF and EGFR inhibition in BRAFV600E colorectal tumors.

Nature cancer

Ruiz-Saenz A, Atreya CE, Wang C, Pan B, Dreyer CA, Brunen D, Prahallad A, Muñoz DP, Ramms DJ, Burghi V, Spassov DS, Fewings E, Hwang YC, Cowdrey C, Moelders C, Schwarzer C, Wolf DM, Hann B, VandenBerg SR, Shokat K, Moasser MM, Bernards R, Gutkind JS, van 't Veer LJ, Coppé JP

A Small Molecule Reacts with the p53 Somatic Mutant Y220C to Rescue Wild-type Thermal Stability.

Cancer discovery

Guiley KZ, Shokat KM

IFITM proteins assist cellular uptake of diverse linked chemotypes.

Science (New York, N.Y.)

Lou K, Wassarman DR, Yang T, Paung Y, Zhang Z, O'Loughlin TA, Moore MK, Egan RK, Greninger P, Benes CH, Seeliger MA, Taunton J, Gilbert LA, Shokat KM

Probing the KRas Switch II Groove by Fluorine NMR Spectroscopy.

ACS chemical biology

Peacock DM, Kelly MJS, Shokat KM

State-selective modulation of heterotrimeric Gαs signaling with macrocyclic peptides.

Cell

Dai SA, Hu Q, Gao R, Blythe EE, Touhara KK, Peacock H, Zhang Z, von Zastrow M, Suga H, Shokat KM

Brain-restricted mTOR inhibition with binary pharmacology.

Nature

Zhang Z, Fan Q, Luo X, Lou K, Weiss WA, Shokat KM

Cold shock domain-containing protein E1 is a posttranscriptional regulator of the LDL receptor.

Science translational medicine

Smith GA, Padmanabhan A, Lau BH, Pampana A, Li L, Lee CY, Pelonero A, Nishino T, Sadagopan N, Xia VQ, Jain R, Natarajan P, Wu RS, Black BL, Srivastava D, Shokat KM, Chorba JS

A covalent inhibitor of K-Ras(G12C) induces MHC class I presentation of haptenated peptide neoepitopes targetable by immunotherapy.

Cancer cell

Zhang Z, Rohweder PJ, Ongpipattanakul C, Basu K, Bohn MF, Dugan EJ, Steri V, Hann B, Shokat KM, Craik CS

Tissue-restricted inhibition of mTOR using chemical genetics.

Proceedings of the National Academy of Sciences of the United States of America

Wassarman DR, Bankapalli K, Pallanck LJ, Shokat KM

Chemoselective Covalent Modification of K-Ras(G12R) with a Small Molecule Electrophile.

Journal of the American Chemical Society

Zhang Z, Morstein J, Ecker AK, Guiley KZ, Shokat KM

Chemical acylation of an acquired serine suppresses oncogenic signaling of K-Ras(G12S).

Nature chemical biology

Zhang Z, Guiley KZ, Shokat KM

CD74-NRG1 Fusions Are Oncogenic In Vivo and Induce Therapeutically Tractable ERBB2:ERBB3 Heterodimerization.

Molecular cancer therapeutics

Werr L, Plenker D, Dammert MA, Lorenz C, Brägelmann J, Tumbrink HL, Klein S, Schmitt A, Büttner R, Persigehl T, Shokat KM, Wunderlich FT, Schram AM, Peifer M, Sos ML, Reinhardt HC, Thomas RK

Publisher Correction: Evolution of enhanced innate immune evasion by SARS-CoV-2.

Nature

Thorne LG, Bouhaddou M, Reuschl AK, Zuliani-Alvarez L, Polacco B, Pelin A, Batra J, Whelan MVX, Hosmillo M, Fossati A, Ragazzini R, Jungreis I, Ummadi M, Rojc A, Turner J, Bischof ML, Obernier K, Braberg H, Soucheray M, Richards A, Chen KH, Harjai B, Memon D, Hiatt J, Rosales R, McGovern BL, Jahun A, Fabius JM, White K, Goodfellow IG, Takeuchi Y, Bonfanti P, Shokat K, Jura N, Verba K, Noursadeghi M, Beltrao P, Kellis M, Swaney DL, García-Sastre A, Jolly C, Towers GJ, Krogan NJ

KRAS is vulnerable to reversible switch-II pocket engagement in cells.

Nature chemical biology

Vasta JD, Peacock DM, Zheng Q, Walker JA, Zhang Z, Zimprich CA, Thomas MR, Beck MT, Binkowski BF, Corona CR, Robers MB, Shokat KM

Drugging the Next Undruggable KRAS Allele-Gly12Asp.

Journal of medicinal chemistry

Zheng Q, Peacock DM, Shokat KM

Drugging the undruggable: Ross Cagan interviews Kevan Shokat.

Disease models & mechanisms

Cagan R, Shokat K

Targeting a splicing-mediated drug resistance mechanism in prostate cancer by inhibiting transcriptional regulation by PKCβ1.

Oncogene

Melnyk JE, Steri V, Nguyen HG, Hwang YC, Gordan JD, Hann B, Feng FY, Shokat KM

Evolution of enhanced innate immune evasion by SARS-CoV-2.

Nature

Thorne LG, Bouhaddou M, Reuschl AK, Zuliani-Alvarez L, Polacco B, Pelin A, Batra J, Whelan MVX, Hosmillo M, Fossati A, Ragazzini R, Jungreis I, Ummadi M, Rojc A, Turner J, Bischof ML, Obernier K, Braberg H, Soucheray M, Richards A, Chen KH, Harjai B, Memon D, Hiatt J, Rosales R, McGovern BL, Jahun A, Fabius JM, White K, Goodfellow IG, Takeuchi Y, Bonfanti P, Shokat K, Jura N, Verba K, Noursadeghi M, Beltrao P, Kellis M, Swaney DL, García-Sastre A, Jolly C, Towers GJ, Krogan NJ

Dissecting the biology of mTORC1 beyond rapamycin.

Science signaling

Yang G, Francis D, Krycer JR, Larance M, Zhang Z, Novotny CJ, Diaz-Vegas A, Shokat KM, James DE

Brain-specific inhibition of mTORC1 eliminates side effects resulting from mTORC1 blockade in the periphery and reduces alcohol intake in mice.

Nature communications

Ehinger Y, Zhang Z, Phamluong K, Soneja D, Shokat KM, Ron D

Drug-induced phospholipidosis confounds drug repurposing for SARS-CoV-2.

Science (New York, N.Y.)

Tummino TA, Rezelj VV, Fischer B, Fischer A, O'Meara MJ, Monel B, Vallet T, White KM, Zhang Z, Alon A, Schadt H, O'Donnell HR, Lyu J, Rosales R, McGovern BL, Rathnasinghe R, Jangra S, Schotsaert M, Galarneau JR, Krogan NJ, Urban L, Shokat KM, Kruse AC, García-Sastre A, Schwartz O, Moretti F, Vignuzzi M, Pognan F, Shoichet BK

Evolution of enhanced innate immune evasion by the SARS-CoV-2 B.1.1.7 UK variant.

bioRxiv : the preprint server for biology

Thorne LG, Bouhaddou M, Reuschl AK, Zuliani-Alvarez L, Polacco B, Pelin A, Batra J, Whelan MVX, Ummadi M, Rojc A, Turner J, Obernier K, Braberg H, Soucheray M, Richards A, Chen KH, Harjai B, Memon D, Hosmillo M, Hiatt J, Jahun A, Goodfellow IG, Fabius JM, Shokat K, Jura N, Verba K, Noursadeghi M, Beltrao P, Swaney DL, Garcia-Sastre A, Jolly C, Towers GJ, Krogan NJ

Phospholipidosis is a shared mechanism underlying the in vitro antiviral activity of many repurposed drugs against SARS-CoV-2.

bioRxiv : the preprint server for biology

Tummino TA, Rezelj VV, Fischer B, Fischer A, O'Meara MJ, Monel B, Vallet T, Zhang Z, Alon A, O'Donnell HR, Lyu J, Schadt H, White KM, Krogan NJ, Urban L, Shokat KM, Kruse AC, García-Sastre A, Schwartz O, Moretti F, Vignuzzi M, Pognan F, Shoichet BK

Spermatogonial Stem Cell Numbers Are Reduced by Transient Inhibition of GDNF Signaling but Restored by Self-Renewing Replication when Signaling Resumes.

Stem cell reports

Parker N, Laychur A, Sukwani M, Orwig KE, Oatley JM, Zhang C, Rutaganira FU, Shokat K, Wright WW

Host-directed therapies against early-lineage SARS-CoV-2 retain efficacy against B.1.1.7 variant.

bioRxiv : the preprint server for biology

Reuschl AK, Thorne LG, Zuliani-Alvarez L, Bouhaddou M, Obernier K, Hiatt J, Soucheray M, Turner J, Fabius JM, Nguyen GT, Swaney DL, Rosales R, White KM, Avilés P, Kirby IT, Melnyk JE, Shi Y, Zhang Z, Shokat KM, García-Sastre A, Jolly C, Towers GJ, Krogan NJ

Drugging the "Undruggable" MYCN Oncogenic Transcription Factor: Overcoming Previous Obstacles to Impact Childhood Cancers.

Cancer research

Wolpaw AJ, Bayliss R, Büchel G, Dang CV, Eilers M, Gustafson WC, Hansen GH, Jura N, Knapp S, Lemmon MA, Levens D, Maris JM, Marmorstein R, Metallo SJ, Park JR, Penn LZ, Rape M, Roussel MF, Shokat KM, Tansey WP, Verba KA, Vos SM, Weiss WA, Wolf E, Mossé YP

Plitidepsin has potent preclinical efficacy against SARS-CoV-2 by targeting the host protein eEF1A.

Science (New York, N.Y.)

White KM, Rosales R, Yildiz S, Kehrer T, Miorin L, Moreno E, Jangra S, Uccellini MB, Rathnasinghe R, Coughlan L, Martinez-Romero C, Batra J, Rojc A, Bouhaddou M, Fabius JM, Obernier K, Dejosez M, Guillén MJ, Losada A, Avilés P, Schotsaert M, Zwaka T, Vignuzzi M, Shokat KM, Krogan NJ, García-Sastre A

Comparative host-coronavirus protein interaction networks reveal pan-viral disease mechanisms.

Science (New York, N.Y.)

Gordon DE, Hiatt J, Bouhaddou M, Rezelj VV, Ulferts S, Braberg H, Jureka AS, Obernier K, Guo JZ, Batra J, Kaake RM, Weckstein AR, Owens TW, Gupta M, Pourmal S, Titus EW, Cakir M, Soucheray M, McGregor M, Cakir Z, Jang G, O'Meara MJ, Tummino TA, Zhang Z, Foussard H, Rojc A, Zhou Y, Kuchenov D, Hüttenhain R, Xu J, Eckhardt M, Swaney DL, Fabius JM, Ummadi M, Tutuncuoglu B, Rathore U, Modak M, Haas P, Haas KM, Naing ZZC, Pulido EH, Shi Y, Barrio-Hernandez I, Memon D, Petsalaki E, Dunham A, Marrero MC, Burke D, Koh C, Vallet T, Silvas JA, Azumaya CM, Billesbølle C, Brilot AF, Campbell MG, Diallo A, Dickinson MS, Diwanji D, Herrera N, Hoppe N, Kratochvil HT, Liu Y, Merz GE, Moritz M, Nguyen HC, Nowotny C, Puchades C, Rizo AN, Schulze-Gahmen U, Smith AM, Sun M, Young ID, Zhao J, Asarnow D, Biel J, Bowen A, Braxton JR, Chen J, Chio CM, Chio US, Deshpande I, Doan L, Faust B, Flores S, Jin M, Kim K, Lam VL, Li F, Li J, Li YL, Li Y, Liu X, Lo M, Lopez KE, Melo AA, Moss FR, Nguyen P, Paulino J, Pawar KI, Peters JK, Pospiech TH, Safari M, Sangwan S, Schaefer K, Thomas PV, Thwin AC, Trenker R, Tse E, Tsui TKM, Wang F, Whitis N, Yu Z, Zhang K, Zhang Y, Zhou F, Saltzberg D, QCRG Structural Biology Consortium, Hodder AJ, Shun-Shion AS, Williams DM, White KM, Rosales R, Kehrer T, Miorin L, Moreno E, Patel AH, Rihn S, Khalid MM, Vallejo-Gracia A, Fozouni P, Simoneau CR, Roth TL, Wu D, Karim MA, Ghoussaini M, Dunham I, Berardi F, Weigang S, Chazal M, Park J, Logue J, McGrath M, Weston S, Haupt R, Hastie CJ, Elliott M, Brown F, Burness KA, Reid E, Dorward M, Johnson C, Wilkinson SG, Geyer A, Giesel DM, Baillie C, Raggett S, Leech H, Toth R, Goodman N, Keough KC, Lind AL, Zoonomia Consortium, Klesh RJ, Hemphill KR, Carlson-Stevermer J, Oki J, Holden K, Maures T, Pollard KS, Sali A, Agard DA, Cheng Y, Fraser JS, Frost A, Jura N, Kortemme T, Manglik A, Southworth DR, Stroud RM, Alessi DR, Davies P, Frieman MB, Ideker T, Abate C, Jouvenet N, Kochs G, Shoichet B, Ott M, Palmarini M, Shokat KM, García-Sastre A, Rassen JA, Grosse R, Rosenberg OS, Verba KA, Basler CF, Vignuzzi M, Peden AA, Beltrao P, Krogan NJ

GTP-State-Selective Cyclic Peptide Ligands of K-Ras(G12D) Block Its Interaction with Raf.

ACS central science

Zhang Z, Gao R, Hu Q, Peacock H, Peacock DM, Dai S, Shokat KM, Suga H

The splicing modulator sulfonamide indisulam reduces AR-V7 in prostate cancer cells.

Bioorganic & medicinal chemistry

Melnyk JE, Steri V, Nguyen HG, Hann B, Feng FY, Shokat KM

The Global Phosphorylation Landscape of SARS-CoV-2 Infection.

Cell

Bouhaddou M, Memon D, Meyer B, White KM, Rezelj VV, Correa Marrero M, Polacco BJ, Melnyk JE, Ulferts S, Kaake RM, Batra J, Richards AL, Stevenson E, Gordon DE, Rojc A, Obernier K, Fabius JM, Soucheray M, Miorin L, Moreno E, Koh C, Tran QD, Hardy A, Robinot R, Vallet T, Nilsson-Payant BE, Hernandez-Armenta C, Dunham A, Weigang S, Knerr J, Modak M, Quintero D, Zhou Y, Dugourd A, Valdeolivas A, Patil T, Li Q, Hüttenhain R, Cakir M, Muralidharan M, Kim M, Jang G, Tutuncuoglu B, Hiatt J, Guo JZ, Xu J, Bouhaddou S, Mathy CJP, Gaulton A, Manners EJ, Félix E, Shi Y, Goff M, Lim JK, McBride T, O'Neal MC, Cai Y, Chang JCJ, Broadhurst DJ, Klippsten S, De Wit E, Leach AR, Kortemme T, Shoichet B, Ott M, Saez-Rodriguez J, tenOever BR, Mullins RD, Fischer ER, Kochs G, Grosse R, García-Sastre A, Vignuzzi M, Johnson JR, Shokat KM, Swaney DL, Beltrao P, Krogan NJ

Unbiased Proteomic Profiling Uncovers a Targetable GNAS/PKA/PP2A Axis in Small Cell Lung Cancer Stem Cells.

Cancer cell

Coles GL, Cristea S, Webber JT, Levin RS, Moss SM, He A, Sangodkar J, Hwang YC, Arand J, Drainas AP, Mooney NA, Demeter J, Spradlin JN, Mauch B, Le V, Shue YT, Ko JH, Lee MC, Kong C, Nomura DK, Ohlmeyer M, Swaney DL, Krogan NJ, Jackson PK, Narla G, Gordan JD, Shokat KM, Sage J

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.

Nature

Gordon DE, Jang GM, Bouhaddou M, Xu J, Obernier K, White KM, O'Meara MJ, Rezelj VV, Guo JZ, Swaney DL, Tummino TA, Hüttenhain R, Kaake RM, Richards AL, Tutuncuoglu B, Foussard H, Batra J, Haas K, Modak M, Kim M, Haas P, Polacco BJ, Braberg H, Fabius JM, Eckhardt M, Soucheray M, Bennett MJ, Cakir M, McGregor MJ, Li Q, Meyer B, Roesch F, Vallet T, Mac Kain A, Miorin L, Moreno E, Naing ZZC, Zhou Y, Peng S, Shi Y, Zhang Z, Shen W, Kirby IT, Melnyk JE, Chorba JS, Lou K, Dai SA, Barrio-Hernandez I, Memon D, Hernandez-Armenta C, Lyu J, Mathy CJP, Perica T, Pilla KB, Ganesan SJ, Saltzberg DJ, Rakesh R, Liu X, Rosenthal SB, Calviello L, Venkataramanan S, Liboy-Lugo J, Lin Y, Huang XP, Liu Y, Wankowicz SA, Bohn M, Safari M, Ugur FS, Koh C, Savar NS, Tran QD, Shengjuler D, Fletcher SJ, O'Neal MC, Cai Y, Chang JCJ, Broadhurst DJ, Klippsten S, Sharp PP, Wenzell NA, Kuzuoglu-Ozturk D, Wang HY, Trenker R, Young JM, Cavero DA, Hiatt J, Roth TL, Rathore U, Subramanian A, Noack J, Hubert M, Stroud RM, Frankel AD, Rosenberg OS, Verba KA, Agard DA, Ott M, Emerman M, Jura N, von Zastrow M, Verdin E, Ashworth A, Schwartz O, d'Enfert C, Mukherjee S, Jacobson M, Malik HS, Fujimori DG, Ideker T, Craik CS, Floor SN, Fraser JS, Gross JD, Sali A, Roth BL, Ruggero D, Taunton J, Kortemme T, Beltrao P, Vignuzzi M, García-Sastre A, Shokat KM, Shoichet BK, Krogan NJ

Betacellulin drives therapy resistance in glioblastoma.

Neuro-Oncology

Fan Q, An Z, Wong RA, Luo X, Lu ED, Baldwin A, Mayekar MK, Haderk F, Shokat KM, Bivona TG, Weiss WA

A SARS-CoV-2-Human Protein-Protein Interaction Map Reveals Drug Targets and Potential Drug-Repurposing.

bioRxiv : the preprint server for biology

Gordon DE, Jang GM, Bouhaddou M, Xu J, Obernier K, O'Meara MJ, Guo JZ, Swaney DL, Tummino TA, Hüttenhain R, Kaake RM, Richards AL, Tutuncuoglu B, Foussard H, Batra J, Haas K, Modak M, Kim M, Haas P, Polacco BJ, Braberg H, Fabius JM, Eckhardt M, Soucheray M, Bennett MJ, Cakir M, McGregor MJ, Li Q, Naing ZZC, Zhou Y, Peng S, Kirby IT, Melnyk JE, Chorba JS, Lou K, Dai SA, Shen W, Shi Y, Zhang Z, Barrio-Hernandez I, Memon D, Hernandez-Armenta C, Mathy CJP, Perica T, Pilla KB, Ganesan SJ, Saltzberg DJ, Ramachandran R, Liu X, Rosenthal SB, Calviello L, Venkataramanan S, Lin Y, Wankowicz SA, Bohn M, Trenker R, Young JM, Cavero D, Hiatt J, Roth T, Rathore U, Subramanian A, Noack J, Hubert M, Roesch F, Vallet T, Meyer B, White KM, Miorin L, Agard D, Emerman M, Ruggero D, García-Sastre A, Jura N, von Zastrow M, Taunton J, Schwartz O, Vignuzzi M, d'Enfert C, Mukherjee S, Jacobson M, Malik HS, Fujimori DG, Ideker T, Craik CS, Floor S, Fraser JS, Gross J, Sali A, Kortemme T, Beltrao P, Shokat K, Shoichet BK, Krogan NJ

PI4KIIIβ is a therapeutic target in chromosome 1q-amplified lung adenocarcinoma.

Science translational medicine

Tan X, Banerjee P, Pham EA, Rutaganira FUN, Basu K, Bota-Rabassedas N, Guo HF, Grzeskowiak CL, Liu X, Yu J, Shi L, Peng DH, Rodriguez BL, Zhang J, Zheng V, Duose DY, Solis LM, Mino B, Raso MG, Behrens C, Wistuba II, Scott KL, Smith M, Nguyen K, Lam G, Choong I, Mazumdar A, Hill JL, Gibbons DL, Brown PH, Russell WK, Shokat K, Creighton CJ, Glenn JS, Kurie JM

p27 allosterically activates cyclin-dependent kinase 4 and antagonizes palbociclib inhibition.

Science (New York, N.Y.)

Guiley KZ, Stevenson JW, Lou K, Barkovich KJ, Kumarasamy V, Wijeratne TU, Bunch KL, Tripathi S, Knudsen ES, Witkiewicz AK, Shokat KM, Rubin SM

Cooperative Blockade of PKCα and JAK2 Drives Apoptosis in Glioblastoma.

Cancer research

Wong RA, Luo X, Lu M, An Z, Haas-Kogan DA, Phillips JJ, Shokat KM, Weiss WA, Fan QW

p38γ MAPK contributes to left ventricular remodeling after pathologic stress and disinhibits calpain through phosphorylation of calpastatin.

FASEB journal : official publication of the Federation of American Societies for Experimental Biology

Loonat AA, Martin ED, Sarafraz-Shekary N, Tilgner K, Hertz NT, Levin R, Shokat KM, Burlingame AL, Arabacilar P, Uddin S, Thomas M, Marber MS, Clark JE

Bifunctional Small-Molecule Ligands of K-Ras Induce Its Association with Immunophilin Proteins.

Angewandte Chemie (International ed. in English)

Zhang Z, Shokat KM

A Bounty of New Challenging Targets in Oncology for Chemical Discovery.

Biochemistry

Lou K, Gilbert LA, Shokat KM

KRASG12C inhibition produces a driver-limited state revealing collateral dependencies.

Science signaling

Lou K, Steri V, Ge AY, Hwang YC, Yogodzinski CH, Shkedi AR, Choi ALM, Mitchell DC, Swaney DL, Hann B, Gordan JD, Shokat KM, Gilbert LA

Phosphoregulation of the oncogenic protein regulator of cytokinesis 1 (PRC1) by the atypical CDK16/CCNY complex.

Experimental & molecular medicine

Hernández-Ortega S, Sánchez-Botet A, Quandt E, Masip N, Gasa L, Verde G, Jiménez J, Levin RS, Rutaganira FU, Burlingame AL, Wolfgeher D, Ribeiro MPC, Kron SJ, Shokat KM, Clotet J

A Legionella pneumophila Kinase Phosphorylates the Hsp70 Chaperone Family to Inhibit Eukaryotic Protein Synthesis.

Cell host & microbe

Moss SM, Taylor IR, Ruggero D, Gestwicki JE, Shokat KM, Mukherjee S

Chronic TGF-β exposure drives stabilized EMT, tumor stemness, and cancer drug resistance with vulnerability to bitopic mTOR inhibition.

Science signaling

Katsuno Y, Meyer DS, Zhang Z, Shokat KM, Akhurst RJ, Miyazono K, Derynck R

Chemically reprogramming the phospho-transfer reaction to crosslink protein kinases to their substrates.

Protein science : a publication of the Protein Society

Wong AW, Urisman A, Burlingame AL, Shokat KM

Type II Kinase Inhibitors Targeting Cys-Gatekeeper Kinases Display Orthogonality with Wild Type and Ala/Gly-Gatekeeper Kinases.

ACS chemical biology

Ocasio CA, Warkentin AA, McIntyre PJ, Barkovich KJ, Vesely C, Spencer J, Shokat KM, Bayliss R

Chemical genetic inhibition of DEAD-box proteins using covalent complementarity.

Nucleic Acids Research

Barkovich KJ, Moore MK, Hu Q, Shokat KM

A Patient-derived Xenograft Model of Pancreatic Neuroendocrine Tumors Identifies Sapanisertib as a Possible New Treatment for Everolimus-resistant Tumors.

Molecular cancer therapeutics

Chamberlain CE, German MS, Yang K, Wang J, VanBrocklin H, Regan M, Shokat KM, Ducker GS, Kim GE, Hann B, Donner DB, Warren RS, Venook AP, Bergsland EK, Lee D, Wang Y, Nakakura EK

A High-Throughput Luciferase Assay to Evaluate Proteolysis of the Single-Turnover Protease PCSK9.

Journal of visualized experiments : JoVE

Chorba JS, Galvan AM, Shokat KM

Kinome rewiring reveals AURKA limits PI3K-pathway inhibitor efficacy in breast cancer.

Nature chemical biology

Donnella HJ, Webber JT, Levin RS, Camarda R, Momcilovic O, Bayani N, Shah KN, Korkola JE, Shokat KM, Goga A, Gordan JD, Bandyopadhyay S

Comprehensive analysis of T cell leukemia signals reveals heterogeneity in the PI3 kinase-Akt pathway and limitations of PI3 kinase inhibitors as monotherapy.

PloS one

Ksionda O, Mues M, Wandler AM, Donker L, Tenhagen M, Jun J, Ducker GS, Matlawska-Wasowska K, Shannon K, Shokat KM, Roose JP

Stepwise processing analyses of the single-turnover PCSK9 protease reveal its substrate sequence specificity and link clinical genotype to lipid phenotype.

The Journal of biological chemistry

Chorba JS, Galvan AM, Shokat KM

Disease-Causing Mutations in the G Protein Gαs Subvert the Roles of GDP and GTP.

Cell

Hu Q, Shokat KM

Novel K-Ras G12C Switch-II Covalent Binders Destabilize Ras and Accelerate Nucleotide Exchange.

Journal of chemical information and modeling

Nnadi CI, Jenkins ML, Gentile DR, Bateman LA, Zaidman D, Balius TE, Nomura DK, Burke JE, Shokat KM, London N

Stepwise processing analyses of the single-turnover PCSK9 protease reveal its substrate sequence specificity and link clinical genotype to lipid phenotype.

The Journal of biological chemistry

Chorba JS, Galvan AM, Shokat KM

Ras Binder Induces a Modified Switch-II Pocket in GTP and GDP States.

Cell chemical biology

Gentile DR, Rathinaswamy MK, Jenkins ML, Moss SM, Siempelkamp BD, Renslo AR, Burke JE, Shokat KM

Inhibition of Calcium Dependent Protein Kinase 1 (CDPK1) by Pyrazolopyrimidine Analogs Decreases Establishment and Reoccurrence of Central Nervous System Disease by Toxoplasma gondii.

Journal of medicinal chemistry

Rutaganira FU, Barks J, Dhason MS, Wang Q, Lopez MS, Long S, Radke JB, Jones NG, Maddirala AR, Janetka JW, El Bakkouri M, Hui R, Shokat KM, Sibley LD

A new generation of mTORC1 inhibitor attenuates alcohol intake and reward in mice.

Addiction biology

Morisot N, Novotny CJ, Shokat KM, Ron D

Drugging the 'undruggable' cancer targets.

Nature reviews. Cancer

Dang CV, Reddy EP, Shokat KM, Soucek L

Farnesyltransferase-Mediated Delivery of a Covalent Inhibitor Overcomes Alternative Prenylation to Mislocalize K-Ras.

ACS chemical biology

Novotny CJ, Hamilton GL, McCormick F, Shokat KM

Expanding the Scope of Electrophiles Capable of Targeting K-Ras Oncogenes.

Biochemistry

McGregor LM, Jenkins ML, Kerwin C, Burke JE, Shokat KM

Drugging the catalytically inactive state of RET kinase in RET-rearranged tumors.

Science translational medicine

Plenker D, Riedel M, Brägelmann J, Dammert MA, Chauhan R, Knowles PP, Lorenz C, Keul M, Bührmann M, Pagel O, Tischler V, Scheel AH, Schütte D, Song Y, Stark J, Mrugalla F, Alber Y, Richters A, Engel J, Leenders F, Heuckmann JM, Wolf J, Diebold J, Pall G, Peifer M, Aerts M, Gevaert K, Zahedi RP, Buettner R, Shokat KM, McDonald NQ, Kast SM, Gautschi O, Thomas RK, Sos ML

Site-specific incorporation of phosphotyrosine using an expanded genetic code.

Nature chemical biology

Hoppmann C, Wong A, Yang B, Li S, Hunter T, Shokat KM, Wang L

Ablation of PI3K blocks BCR-ABL leukemogenesis in mice, and a dual PI3K/mTOR inhibitor prevents expansion of human BCR-ABL+ leukemia cells.

The Journal of clinical investigation

Kharas MG, Janes MR, Scarfone VM, Lilly MB, Knight ZA, Shokat KM, Fruman DA

Discovery of nitrate-CPK-NLP signalling in central nutrient-growth networks.

Nature

Liu KH, Niu Y, Konishi M, Wu Y, Du H, Sun Chung H, Li L, Boudsocq M, McCormack M, Maekawa S, Ishida T, Zhang C, Shokat K, Yanagisawa S, Sheen J

Long-term oral kinetin does not protect against α-synuclein-induced neurodegeneration in rodent models of Parkinson's disease.

Neurochemistry international

Orr AL, Rutaganira FU, de Roulet D, Huang EJ, Hertz NT, Shokat KM, Nakamura K

A Kinase Inhibitor Targeted to mTORC1 Drives Regression in Glioblastoma.

Cancer cell

Fan Q, Aksoy O, Wong RA, Ilkhanizadeh S, Novotny CJ, Gustafson WC, Truong AY, Cayanan G, Simonds EF, Haas-Kogan D, Phillips JJ, Nicolaides T, Okaniwa M, Shokat KM, Weiss WA

INPP4B and PTEN Loss Leads to PI-3,4-P2 Accumulation and Inhibition of PI3K in TNBC.

Molecular cancer research : MCR

Reed DE, Shokat KM

An Optimized Chromatographic Strategy for Multiplexing In Parallel Reaction Monitoring Mass Spectrometry: Insights from Quantitation of Activated Kinases.

Molecular & cellular proteomics : MCP

Urisman A, Levin RS, Gordan JD, Webber JT, Hernandez H, Ishihama Y, Shokat KM, Burlingame AL

Endosomal Phosphatidylinositol 3-Kinase Is Essential for Canonical GPCR Signaling.

Molecular pharmacology

Uchida Y, Rutaganira FU, Jullié D, Shokat KM, von Zastrow M

Discovery of new substrates of the elongation factor-2 kinase suggests a broader role in the cellular nutrient response.

Cellular signalling

Lazarus MB, Levin RS, Shokat KM

Overcoming resistance to HER2 inhibitors through state-specific kinase binding.

Nature chemical biology

Novotny CJ, Pollari S, Park JH, Lemmon MA, Shen W, Shokat KM

From Powerful Review Articles to Research Breakthroughs.

Cell chemical biology

Kostic M, Crews CM, Hertweck C, Shokat K, Suga H

Inhibition of Carbonyl Reductase 1 Safely Improves the Efficacy of Doxorubicin in Breast Cancer Treatment.

Antioxidants & redox signaling

Jo A, Choi TG, Jo YH, Jyothi KR, Nguyen MN, Kim JH, Lim S, Shahid M, Akter S, Lee S, Lee KH, Kim W, Cho H, Lee J, Shokat KM, Yoon KS, Kang I, Ha J, Kim SS

Innate immunity kinase TAK1 phosphorylates Rab1 on a hotspot for posttranslational modifications by host and pathogen.

Proceedings of the National Academy of Sciences of the United States of America

Levin RS, Hertz NT, Burlingame AL, Shokat KM, Mukherjee S

Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design.

Nature reviews. Drug discovery

Ostrem JM, Shokat KM

Synthetic Lethal Targeting of ARID1A-Mutant Ovarian Clear Cell Tumors with Dasatinib.

Molecular cancer therapeutics

Miller RE, Brough R, Bajrami I, Williamson CT, McDade S, Campbell J, Kigozi A, Rafiq R, Pemberton H, Natrajan R, Joel J, Astley H, Mahoney C, Moore JD, Torrance C, Gordan JD, Webber JT, Levin RS, Shokat KM, Bandyopadhyay S, Lord CJ, Ashworth A

Isocitrate Dehydrogenase Mutations Confer Dasatinib Hypersensitivity and SRC Dependence in Intrahepatic Cholangiocarcinoma.

Cancer discovery

Saha SK, Gordan JD, Kleinstiver BP, Vu P, Najem MS, Yeo JC, Shi L, Kato Y, Levin RS, Webber JT, Damon LJ, Egan RK, Greninger P, McDermott U, Garnett MJ, Jenkins RL, Rieger-Christ KM, Sullivan TB, Hezel AF, Liss AS, Mizukami Y, Goyal L, Ferrone CR, Zhu AX, Joung JK, Shokat KM, Benes CH, Bardeesy N

Overcoming mTOR resistance mutations with a new-generation mTOR inhibitor.

Nature

Rodrik-Outmezguine VS, Okaniwa M, Yao Z, Novotny CJ, McWhirter C, Banaji A, Won H, Wong W, Berger M, de Stanchina E, Barratt DG, Cosulich S, Klinowska T, Rosen N, Shokat KM

Multistep Compositional Remodeling of Supported Lipid Membranes by Interfacially Active Phosphatidylinositol Kinases.

Analytical chemistry

Tabaei SR, Guo F, Rutaganira FU, Vafaei S, Choong I, Shokat KM, Glenn JS, Cho NJ

N-Myc Drives Neuroendocrine Prostate Cancer Initiated from Human Prostate Epithelial Cells.

Cancer cell

Lee JK, Phillips JW, Smith BA, Park JW, Stoyanova T, McCaffrey EF, Baertsch R, Sokolov A, Meyerowitz JG, Mathis C, Cheng D, Stuart JM, Shokat KM, Gustafson WC, Huang J, Witte ON

Our Advisors, Our Ambassadors, Our Editorial Board Members.

Cell chemical biology

Kostic M, Crews CM, Hertweck C, Shokat K, Suga H

Design and Structural Characterization of Potent and Selective Inhibitors of Phosphatidylinositol 4 Kinase IIIβ.

Journal of medicinal chemistry

Rutaganira FU, Fowler ML, McPhail JA, Gelman MA, Nguyen K, Xiong A, Dornan GL, Tavshanjian B, Glenn JS, Shokat KM, Burke JE

Voices of Chemical Biology: Charting the Next Decade.

Cell chemical biology

Kostic M, Crews CM, Hertweck C, Shokat K, Suga H

Using hydrogen deuterium exchange mass spectrometry to engineer optimized constructs for crystallization of protein complexes: Case study of PI4KIIIβ with Rab11.

Protein science : a publication of the Protein Society

Fowler ML, McPhail JA, Jenkins ML, Masson GR, Rutaganira FU, Shokat KM, Williams RL, Burke JE

Cell Chemical Biology: Home of Exciting Chemical Biology.

Cell chemical biology

Kostic M, Crews CM, Hertweck C, Shokat K, Suga H

P-TEFb regulation of transcription termination factor Xrn2 revealed by a chemical genetic screen for Cdk9 substrates.

Genes & development

Sansó M, Levin RS, Lipp JJ, Wang VY, Greifenberg AK, Quezada EM, Ali A, Ghosh A, Larochelle S, Rana TM, Geyer M, Tong L, Shokat KM, Fisher RP

Analog sensitive chemical inhibition of the DEAD-box protein DDX3.

Protein science : a publication of the Protein Society

Floor SN, Barkovich KJ, Condon KJ, Shokat KM, Doudna JA

Inhibition of Calcium-Dependent Protein Kinase 1 (CDPK1) In Vitro by Pyrazolopyrimidine Derivatives Does Not Correlate with Sensitivity of Cryptosporidium parvum Growth in Cell Culture.

Antimicrobial agents and chemotherapy

Kuhlenschmidt TB, Rutaganira FU, Long S, Tang K, Shokat KM, Kuhlenschmidt MS, Sibley LD

Discovery and functional characterization of a neomorphic PTEN mutation.

Proceedings of the National Academy of Sciences of the United States of America

Costa HA, Leitner MG, Sos ML, Mavrantoni A, Rychkova A, Johnson JR, Newton BW, Yee MC, De La Vega FM, Ford JM, Krogan NJ, Shokat KM, Oliver D, Halaszovich CR, Bustamante CD

Identification of AMPK Phosphorylation Sites Reveals a Network of Proteins Involved in Cell Invasion and Facilitates Large-Scale Substrate Prediction.

Cell metabolism

Schaffer BE, Levin RS, Hertz NT, Maures TJ, Schoof ML, Hollstein PE, Benayoun BA, Banko MR, Shaw RJ, Shokat KM, Brunet A

Small molecule inhibition of Csk alters affinity recognition by T cells.

eLife

Manz BN, Tan YX, Courtney AH, Rutaganira F, Palmer E, Shokat KM, Weiss A

Discovery and structure of a new inhibitor scaffold of the autophagy initiating kinase ULK1.

Bioorganic & medicinal chemistry

Lazarus MB, Shokat KM

SR protein kinases promote splicing of nonconsensus introns.

Nature structural & molecular biology

Lipp JJ, Marvin MC, Shokat KM, Guthrie C

WNK1-regulated inhibitory phosphorylation of the KCC2 cotransporter maintains the depolarizing action of GABA in immature neurons.

Science signaling

Friedel P, Kahle KT, Zhang J, Hertz N, Pisella LI, Buhler E, Schaller F, Duan J, Khanna AR, Bishop PN, Shokat KM, Medina I

Endoplasmic reticulum stress-independent activation of unfolded protein response kinases by a small molecule ATP-mimic.

eLife

Mendez AS, Alfaro J, Morales-Soto MA, Dar AC, McCullagh E, Gotthardt K, Li H, Acosta-Alvear D, Sidrauski C, Korennykh AV, Bernales S, Shokat KM, Walter P

Downregulation of MYCN through PI3K Inhibition in Mouse Models of Pediatric Neural Cancer.

Frontiers in oncology

Cage TA, Chanthery Y, Chesler L, Grimmer M, Knight Z, Shokat K, Weiss WA, Gustafson WC

Differential genetic interactions of yeast stress response MAPK pathways.

Molecular systems biology

Martin H, Shales M, Fernandez-Piñar P, Wei P, Molina M, Fiedler D, Shokat KM, Beltrao P, Lim W, Krogan NJ

The Tribbles 2 (TRB2) pseudokinase binds to ATP and autophosphorylates in a metal-independent manner.

The Biochemical journal

Bailey FP, Byrne DP, Oruganty K, Eyers CE, Novotny CJ, Shokat KM, Kannan N, Eyers PA

Structure of the human autophagy initiating kinase ULK1 in complex with potent inhibitors.

ACS chemical biology

Lazarus MB, Novotny CJ, Shokat KM

Overcoming myelosuppression due to synthetic lethal toxicity for FLT3-targeted acute myeloid leukemia therapy.

eLife

Warkentin AA, Lopez MS, Lasater EA, Lin K, He BL, Leung AY, Smith CC, Shah NP, Shokat KM

Radiotherapy followed by aurora kinase inhibition targets tumor-propagating cells in human glioblastoma.

Molecular cancer therapeutics

Li N, Maly DJ, Chanthery YH, Sirkis DW, Nakamura JL, Berger MS, James CD, Shokat KM, Weiss WA, Persson AI

Targeting osteosarcoma.

Proceedings of the National Academy of Sciences of the United States of America

Reed DE, Shokat KM

Linking tumor mutations to drug responses via a quantitative chemical-genetic interaction map.

Cancer discovery

Martins MM, Zhou AY, Corella A, Horiuchi D, Yau C, Rakhshandehroo T, Gordan JD, Levin RS, Johnson J, Jascur J, Shales M, Sorrentino A, Cheah J, Clemons PA, Shamji AF, Schreiber SL, Krogan NJ, Shokat KM, McCormick F, Goga A, Bandyopadhyay S

MST3 kinase phosphorylates TAO1/2 to enable Myosin Va function in promoting spine synapse development.

Neuron

Ultanir SK, Yadav S, Hertz NT, Oses-Prieto JA, Claxton S, Burlingame AL, Shokat KM, Jan LY, Jan YN

Reflecting on the past and looking forward to the future of bridging chemistry and biology.

Chemistry & biology

Crews C, Hertweck C, Shokat K, Suga H, Kostic M

The proprotein convertase subtilisin/kexin type 9 (PCSK9) active site and cleavage sequence differentially regulate protein secretion from proteolysis.

The Journal of biological chemistry

Chorba JS, Shokat KM

Drugging MYCN through an allosteric transition in Aurora kinase A.

Cancer cell

Gustafson WC, Meyerowitz JG, Nekritz EA, Chen J, Benes C, Charron E, Simonds EF, Seeger R, Matthay KK, Hertz NT, Eilers M, Shokat KM, Weiss WA

TrkB kinase activity maintains synaptic function and structural integrity at adult neuromuscular junctions.

Journal of applied physiology (Bethesda, Md. : 1985)

Mantilla CB, Stowe JM, Sieck DC, Ermilov LG, Greising SM, Zhang C, Shokat KM, Sieck GC

Responses to glial cell line-derived neurotrophic factor change in mice as spermatogonial stem cells form progenitor spermatogonia which replicate and give rise to more differentiated progeny.

Biology of reproduction

Parker N, Falk H, Singh D, Fidaleo A, Smith B, Lopez MS, Shokat KM, Wright WW

Adipocyte ALK7 links nutrient overload to catecholamine resistance in obesity.

eLife

Guo T, Marmol P, Moliner A, Björnholm M, Zhang C, Shokat KM, Ibanez CF

A sharp T-cell antigen receptor signaling threshold for T-cell proliferation.

Proceedings of the National Academy of Sciences of the United States of America

Au-Yeung BB, Zikherman J, Mueller JL, Ashouri JF, Matloubian M, Cheng DA, Chen Y, Shokat KM, Weiss A

Oncogene mimicry as a mechanism of primary resistance to BRAF inhibitors.

Cell reports

Sos ML, Levin RS, Gordan JD, Oses-Prieto JA, Webber JT, Salt M, Hann B, Burlingame AL, McCormick F, Bandyopadhyay S, Shokat KM

OCT1 is a high-capacity thiamine transporter that regulates hepatic steatosis and is a target of metformin.

Proceedings of the National Academy of Sciences of the United States of America

Chen L, Shu Y, Liang X, Chen EC, Yee SW, Zur AA, Li S, Xu L, Keshari KR, Lin MJ, Chien HC, Zhang Y, Morrissey KM, Liu J, Ostrem J, Younger NS, Kurhanewicz J, Shokat KM, Ashrafi K, Giacomini KM

Quantitative and temporal requirements revealed for Zap70 catalytic activity during T cell development.

Nature immunology

Au-Yeung BB, Melichar HJ, Ross JO, Cheng DA, Zikherman J, Shokat KM, Robey EA, Weiss A

Structures of PI4KIIIβ complexes show simultaneous recruitment of Rab11 and its effectors.

Science (New York, N.Y.)

Burke JE, Inglis AJ, Perisic O, Masson GR, McLaughlin SH, Rutaganira F, Shokat KM, Williams RL

A crosslinker based on a tethered electrophile for mapping kinase-substrate networks.

Chemistry & biology

Riel-Mehan MM, Shokat KM

Methods in Enzymology. Protein kinase inhibitors in research and medicine. Preface.

Methods in enzymology

Shokat KM

The logic and design of analog-sensitive kinases and their small molecule inhibitors.

Methods in enzymology

Lopez MS, Kliegman JI, Shokat KM

Chemical genetics of rapamycin-insensitive TORC2 in S. cerevisiae.

Cell reports

Kliegman JI, Fiedler D, Ryan CJ, Xu YF, Su XY, Thomas D, Caccese MC, Cheng A, Shales M, Rabinowitz JD, Krogan NJ, Shokat KM

Inhibition of the kinase Csk in thymocytes reveals a requirement for actin remodeling in the initiation of full TCR signaling.

Nature immunology

Tan YX, Manz BN, Freedman TS, Zhang C, Shokat KM, Weiss A

PLC-γ and PI3K link cytokines to ERK activation in hematopoietic cells with normal and oncogenic Kras.

Science signaling

Diaz-Flores E, Goldschmidt H, Depeille P, Ng V, Akutagawa J, Krisman K, Crone M, Burgess MR, Williams O, Houseman B, Shokat K, Sampath D, Bollag G, Roose JP, Braun BS, Shannon K

Generation of a patient-derived chordoma xenograft and characterization of the phosphoproteome in a recurrent chordoma.

Journal of neurosurgery

Davies JM, Robinson AE, Cowdrey C, Mummaneni PV, Ducker GS, Shokat KM, Bollen A, Hann B, Phillips JJ

K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions.

Nature

Ostrem JM, Peters U, Sos ML, Wells JA, Shokat KM

Staurosporine-derived inhibitors broaden the scope of analog-sensitive kinase technology.

Journal of the American Chemical Society

Lopez MS, Choy JW, Peters U, Sos ML, Morgan DO, Shokat KM

EGFR phosphorylates tumor-derived EGFRvIII driving STAT3/5 and progression in glioblastoma.

Cancer cell

Fan QW, Cheng CK, Gustafson WC, Charron E, Zipper P, Wong RA, Chen J, Lau J, Knobbe-Thomsen C, Weller M, Jura N, Reifenberger G, Shokat KM, Weiss WA

A neo-substrate that amplifies catalytic activity of parkinson's-disease-related kinase PINK1.

Cell

Hertz NT, Berthet A, Sos ML, Thorn KS, Burlingame AL, Nakamura K, Shokat KM

Structure-guided inhibitor design expands the scope of analog-sensitive kinase technology.

ACS chemical biology

Zhang C, Lopez MS, Dar AC, Ladow E, Finkbeiner S, Yun CH, Eck MJ, Shokat KM

Myc and mTOR converge on a common node in protein synthesis control that confers synthetic lethality in Myc-driven cancers.

Proceedings of the National Academy of Sciences of the United States of America

Pourdehnad M, Truitt ML, Siddiqi IN, Ducker GS, Shokat KM, Ruggero D

PTEN expression is consistent in colorectal cancer primaries and metastases and associates with patient survival.

Cancer medicine

Atreya CE, Sangale Z, Xu N, Matli MR, Tikishvili E, Welbourn W, Stone S, Shokat KM, Warren RS

A Cdk7-Cdk4 T-loop phosphorylation cascade promotes G1 progression.

Molecular cell

Schachter MM, Merrick KA, Larochelle S, Hirschi A, Zhang C, Shokat KM, Rubin SM, Fisher RP

Incomplete inhibition of phosphorylation of 4E-BP1 as a mechanism of primary resistance to ATP-competitive mTOR inhibitors.

Oncogene

Ducker GS, Atreya CE, Simko JP, Hom YK, Matli MR, Benes CH, Hann B, Nakakura EK, Bergsland EK, Donner DB, Settleman J, Shokat KM, Warren RS

Optimizing small molecule inhibitors of calcium-dependent protein kinase 1 to prevent infection by Toxoplasma gondii.

Journal of medicinal chemistry

Lourido S, Zhang C, Lopez MS, Tang K, Barks J, Wang Q, Wildman SA, Shokat KM, Sibley LD

Glucose sensor O-GlcNAcylation coordinates with phosphorylation to regulate circadian clock.

Cell metabolism

Kaasik K, Kivimäe S, Allen JJ, Chalkley RJ, Huang Y, Baer K, Kissel H, Burlingame AL, Shokat KM, Ptácek LJ, Fu YH

News from the Chemistry & Biology editorial team.

Chemistry & biology

Crews C, Shokat K, Suga H, Kostic M

A chemical genetic approach reveals distinct EphB signaling mechanisms during brain development.

Nature neuroscience

Soskis MJ, Ho HY, Bloodgood BL, Robichaux MA, Malik AN, Ataman B, Rubin AA, Zieg J, Zhang C, Shokat KM, Sharma N, Cowan CW, Greenberg ME

Cyclin-dependent kinase control of the initiation-to-elongation switch of RNA polymerase II.

Nature structural & molecular biology

Larochelle S, Amat R, Glover-Cutter K, Sansó M, Zhang C, Allen JJ, Shokat KM, Bentley DL, Fisher RP

Chemical genetics reveals a specific requirement for Cdk2 activity in the DNA damage response and identifies Nbs1 as a Cdk2 substrate in human cells.

PLoS genetics

Wohlbold L, Merrick KA, De S, Amat R, Kim JH, Larochelle S, Allen JJ, Zhang C, Shokat KM, Petrini JH, Fisher RP

A positive feedback loop links opposing functions of P-TEFb/Cdk9 and histone H2B ubiquitylation to regulate transcript elongation in fission yeast.

PLoS genetics

Sansó M, Lee KM, Viladevall L, Jacques PÉ, Pagé V, Nagy S, Racine A, St Amour CV, Zhang C, Shokat KM, Schwer B, Robert F, Fisher RP, Tanny JC

Dual blockade of lipid and cyclin-dependent kinases induces synthetic lethality in malignant glioma.

Proceedings of the National Academy of Sciences of the United States of America

Cheng CK, Gustafson WC, Charron E, Houseman BT, Zunder E, Goga A, Gray NS, Pollok B, Oakes SA, James CD, Shokat KM, Weiss WA, Fan QW

Integrin α9β1 in airway smooth muscle suppresses exaggerated airway narrowing.

The Journal of clinical investigation

Chen C, Kudo M, Rutaganira F, Takano H, Lee C, Atakilit A, Robinett KS, Uede T, Wolters PJ, Shokat KM, Huang X, Sheppard D

The AMP-activated protein kinase Snf1 regulates transcription factor binding, RNA polymerase II activity, and mRNA stability of glucose-repressed genes in Saccharomyces cerevisiae.

The Journal of biological chemistry

Young ET, Zhang C, Shokat KM, Parua PK, Braun KA

In vivo conditions to identify Prkci phosphorylation targets using the analog-sensitive kinase method in zebrafish.

PloS one

Cibrián Uhalte E, Kirchner M, Hellwig N, Allen JJ, Donat S, Shokat KM, Selbach M, Abdelilah-Seyfried S

Carbonyl reductase 1 offers a novel therapeutic target to enhance leukemia treatment by arsenic trioxide.

Cancer research

Jang M, Kim Y, Won H, Lim S, K R J, Dashdorj A, Min YH, Kim SY, Shokat KM, Ha J, Kim SS

Hierarchical modularity and the evolution of genetic interactomes across species.

Molecular cell

Ryan CJ, Roguev A, Patrick K, Xu J, Jahari H, Tong Z, Beltrao P, Shales M, Qu H, Collins SR, Kliegman JI, Jiang L, Kuo D, Tosti E, Kim HS, Edelmann W, Keogh MC, Greene D, Tang C, Cunningham P, Shokat KM, Cagney G, Svensson JP, Guthrie C, Espenshade PJ, Ideker T, Krogan NJ

Chemical genetic discovery of targets and anti-targets for cancer polypharmacology.

Nature

Dar AC, Das TK, Shokat KM, Cagan RL

Orm protein phosphoregulation mediates transient sphingolipid biosynthesis response to heat stress via the Pkh-Ypk and Cdc55-PP2A pathways.

Molecular biology of the cell

Sun Y, Miao Y, Yamane Y, Zhang C, Shokat KM, Takematsu H, Kozutsumi Y, Drubin DG

Separate domains of fission yeast Cdk9 (P-TEFb) are required for capping enzyme recruitment and primed (Ser7-phosphorylated) Rpb1 carboxyl-terminal domain substrate recognition.

Molecular and Cellular Biology

St Amour CV, Sansó M, Bösken CA, Lee KM, Larochelle S, Zhang C, Shokat KM, Geyer M, Fisher RP

Chemical-genetic analysis of cyclin dependent kinase 2 function reveals an important role in cellular transformation by multiple oncogenic pathways.

Proceedings of the National Academy of Sciences of the United States of America

Horiuchi D, Huskey NE, Kusdra L, Wohlbold L, Merrick KA, Zhang C, Creasman KJ, Shokat KM, Fisher RP, Goga A

The in vivo response of stem and other undifferentiated spermatogonia to the reversible inhibition of glial cell line-derived neurotrophic factor signaling in the adult.

Stem cells (Dayton, Ohio)

Savitt J, Singh D, Zhang C, Chen LC, Folmer J, Shokat KM, Wright WW

Kinetics of inhibitor cycling underlie therapeutic disparities between EGFR-driven lung and brain cancers.

Cancer discovery

Barkovich KJ, Hariono S, Garske AL, Zhang J, Blair JA, Fan QW, Shokat KM, Nicolaides T, Weiss WA

Chemical genetic identification of NDR1/2 kinase substrates AAK1 and Rabin8 Uncovers their roles in dendrite arborization and spine development.

Neuron

Ultanir SK, Hertz NT, Li G, Ge WP, Burlingame AL, Pleasure SJ, Shokat KM, Jan LY, Jan YN

The translational landscape of mTOR signalling steers cancer initiation and metastasis.

Nature

Hsieh AC, Liu Y, Edlind MP, Ingolia NT, Janes MR, Sher A, Shi EY, Stumpf CR, Christensen C, Bonham MJ, Wang S, Ren P, Martin M, Jessen K, Feldman ME, Weissman JS, Shokat KM, Rommel C, Ruggero D

Combination of ATP-competitive mammalian target of rapamycin inhibitors with standard chemotherapy for colorectal cancer.

Investigational new drugs

Atreya CE, Ducker GS, Feldman ME, Bergsland EK, Warren RS, Shokat KM

Development of a chemical genetic approach for human aurora B kinase identifies novel substrates of the chromosomal passenger complex.

Molecular & cellular proteomics : MCP

Hengeveld RC, Hertz NT, Vromans MJ, Zhang C, Burlingame AL, Shokat KM, Lens SM

A method to site-specifically incorporate methyl-lysine analogues into recombinant proteins.

Methods in enzymology

Simon MD, Shokat KM

Covalent cross-linking of kinases with their corresponding peptide substrates.

Methods in molecular biology (Clifton, N.J.)

Statsuk AV, Shokat KM

Chemical genetic screen for AMPKα2 substrates uncovers a network of proteins involved in mitosis.

Molecular cell

Banko MR, Allen JJ, Schaffer BE, Wilker EW, Tsou P, White JL, Villén J, Wang B, Kim SR, Sakamoto K, Gygi SP, Cantley LC, Yaffe MB, Shokat KM, Brunet A

Generation of a set of conditional analog-sensitive alleles of essential protein kinases in the fission yeast Schizosaccharomyces pombe.

Cell cycle (Georgetown, Tex.)

Cipak L, Zhang C, Kovacikova I, Rumpf C, Miadokova E, Shokat KM, Gregan J

Genetic deletion of trkB.T1 increases neuromuscular function.

American journal of physiology. Cell physiology

Dorsey SG, Lovering RM, Renn CL, Leitch CC, Liu X, Tallon LJ, Sadzewicz LD, Pratap A, Ott S, Sengamalay N, Jones KM, Barrick C, Fulgenzi G, Becker J, Voelker K, Talmadge R, Harvey BK, Wyatt RM, Vernon-Pitts E, Zhang C, Shokat K, Fraser-Liggett C, Balice-Gordon RJ, Tessarollo L, Ward CW

The Cryptosporidium parvum kinome.

BMC genomics

Artz JD, Wernimont AK, Allali-Hassani A, Zhao Y, Amani M, Lin YH, Senisterra G, Wasney GA, Fedorov O, King O, Roos A, Lunin VV, Qiu W, Finerty P, Hutchinson A, Chau I, von Delft F, MacKenzie F, Lew J, Kozieradzki I, Vedadi M, Schapira M, Zhang C, Shokat K, Heightman T, Hui R

Feedback circuits monitor and adjust basal Lck-dependent events in T cell receptor signaling.

Science signaling

Schoenborn JR, Tan YX, Zhang C, Shokat KM, Weiss A

The mammalian target of rapamycin regulates cholesterol biosynthetic gene expression and exhibits a rapamycin-resistant transcriptional profile.

Proceedings of the National Academy of Sciences of the United States of America

Wang BT, Ducker GS, Barczak AJ, Barbeau R, Erle DJ, Shokat KM

Chemical genetic strategy for targeting protein kinases based on covalent complementarity.

Proceedings of the National Academy of Sciences of the United States of America

Garske AL, Peters U, Cortesi AT, Perez JL, Shokat KM

TrkB and protein kinase Mζ regulate synaptic localization of PSD-95 in developing cortex.

The Journal of neuroscience : the official journal of the Society for Neuroscience

Yoshii A, Murata Y, Kim J, Zhang C, Shokat KM, Constantine-Paton M

Cofactor-mediated conformational control in the bifunctional kinase/RNase Ire1.

BMC biology

Korennykh AV, Egea PF, Korostelev AA, Finer-Moore J, Stroud RM, Zhang C, Shokat KM, Walter P

Structural and functional basis for RNA cleavage by Ire1.

BMC biology

Korennykh AV, Korostelev AA, Egea PF, Finer-Moore J, Stroud RM, Zhang C, Shokat KM, Walter P

Autophagy suppression promotes apoptotic cell death in response to inhibition of the PI3K-mTOR pathway in pancreatic adenocarcinoma.

Journal of molecular medicine (Berlin, Germany)

Mirzoeva OK, Hann B, Hom YK, Debnath J, Aftab D, Shokat K, Korn WM

Switching Cdk2 on or off with small molecules to reveal requirements in human cell proliferation.

Molecular cell

Merrick KA, Wohlbold L, Zhang C, Allen JJ, Horiuchi D, Huskey NE, Goga A, Shokat KM, Fisher RP

A Raf-induced allosteric transition of KSR stimulates phosphorylation of MEK.

Nature

Brennan DF, Dar AC, Hertz NT, Chao WC, Burlingame AL, Shokat KM, Barford D

Chemistry & Biology editors announce changes to the editorial team.

Chemistry & biology

Crews C, Shokat K, Wohlleben W, Kostic M

Dose-dependent effects of focal fractionated irradiation on secondary malignant neoplasms in Nf1 mutant mice.

Cancer research

Nakamura JL, Phong C, Pinarbasi E, Kogan SC, Vandenberg S, Horvai AE, Faddegon BA, Fiedler D, Shokat K, Houseman BT, Chao R, Pieper RO, Shannon K

Sensitizing plant protein kinases to specific inhibition by ATP-competitive molecules.

Methods in molecular biology (Clifton, N.J.)

Salomon D, Zhang C, Shokat KM, Sessa G

The evolution of protein kinase inhibitors from antagonists to agonists of cellular signaling.

Annual review of biochemistry

Dar AC, Shokat KM

Phosphoproteomic analysis reveals interconnected system-wide responses to perturbations of kinases and phosphatases in yeast.

Science signaling

Bodenmiller B, Wanka S, Kraft C, Urban J, Campbell D, Pedrioli PG, Gerrits B, Picotti P, Lam H, Vitek O, Brusniak MY, Roschitzki B, Zhang C, Shokat KM, Schlapbach R, Colman-Lerner A, Nolan GP, Nesvizhskii AI, Peter M, Loewith R, von Mering C, Aebersold R

Rewiring of genetic networks in response to DNA damage.

Science (New York, N.Y.)

Bandyopadhyay S, Mehta M, Kuo D, Sung MK, Chuang R, Jaehnig EJ, Bodenmiller B, Licon K, Copeland W, Shales M, Fiedler D, Dutkowski J, Guénolé A, van Attikum H, Shokat KM, Kolodner RD, Huh WK, Aebersold R, Keogh MC, Krogan NJ, Ideker T

Constitutive mTORC1 activation by a herpesvirus Akt surrogate stimulates mRNA translation and viral replication.

Genes & development

Chuluunbaatar U, Roller R, Feldman ME, Brown S, Shokat KM, Mohr I

Akt and autophagy cooperate to promote survival of drug-resistant glioma.

Science signaling

Fan QW, Cheng C, Hackett C, Feldman M, Houseman BT, Nicolaides T, Haas-Kogan D, James CD, Oakes SA, Debnath J, Shokat KM, Weiss WA

A genetically selective inhibitor demonstrates a function for the kinase Zap70 in regulatory T cells independent of its catalytic activity.

Nature immunology

Au-Yeung BB, Levin SE, Zhang C, Hsu LY, Cheng DA, Killeen N, Shokat KM, Weiss A

A kinase cascade leading to Rab11-FIP5 controls transcytosis of the polymeric immunoglobulin receptor.

Nature cell biology

Su T, Bryant DM, Luton F, Vergés M, Ulrich SM, Hansen KC, Datta A, Eastburn DJ, Burlingame AL, Shokat KM, Mostov KE

GABAA receptor trafficking is regulated by protein kinase C(epsilon) and the N-ethylmaleimide-sensitive factor.

The Journal of neuroscience : the official journal of the Society for Neuroscience

Chou WH, Wang D, McMahon T, Qi ZH, Song M, Zhang C, Shokat KM, Messing RO

Biocompatibility and reduced drug absorption of sol-gel-treated poly(dimethyl siloxane) for microfluidic cell culture applications.

Analytical chemistry

Gomez-Sjoberg R, Leyrat AA, Houseman BT, Shokat K, Quake SR

Human carbonyl reductase 1 upregulated by hypoxia renders resistance to apoptosis in hepatocellular carcinoma cells.

Journal of hepatology

Tak E, Lee S, Lee J, Rashid MA, Kim YW, Park JH, Park WS, Shokat KM, Ha J, Kim SS

Chemical-genomic dissection of the CTD code.

Nature structural & molecular biology

Tietjen JR, Zhang DW, Rodríguez-Molina JB, White BE, Akhtar MS, Heidemann M, Li X, Chapman RD, Shokat K, Keles S, Eick D, Ansari AZ

Mps1 directs the assembly of Cdc20 inhibitory complexes during interphase and mitosis to control M phase timing and spindle checkpoint signaling.

The Journal of Cell Biology

Maciejowski J, George KA, Terret ME, Zhang C, Shokat KM, Jallepalli PV

Synthesis and evaluation of indazole based analog sensitive Akt inhibitors.

Molecular bioSystems

Okuzumi T, Ducker GS, Zhang C, Aizenstein B, Hoffman R, Shokat KM

Calcium-dependent protein kinase 1 is an essential regulator of exocytosis in Toxoplasma.

Nature

Lourido S, Shuman J, Zhang C, Shokat KM, Hui R, Sibley LD

A drug-drug interaction crystallizes a new entry point into the UPR.

Molecular cell

Shokat KM

Chemical genetic inhibition of Mps1 in stable human cell lines reveals novel aspects of Mps1 function in mitosis.

PloS one

Sliedrecht T, Zhang C, Shokat KM, Kops GJ

Shaping development of autophagy inhibitors with the structure of the lipid kinase Vps34.

Science (New York, N.Y.)

Miller S, Tavshanjian B, Oleksy A, Perisic O, Houseman BT, Shokat KM, Williams RL

mTOR complex-2 activates ENaC by phosphorylating SGK1.

Journal of the American Society of Nephrology : JASN

Lu M, Wang J, Jones KT, Ives HE, Feldman ME, Yao LJ, Shokat KM, Ashrafi K, Pearce D

RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF.

Nature

Poulikakos PI, Zhang C, Bollag G, Shokat KM, Rosen N

Genetic dissection of the oncogenic mTOR pathway reveals druggable addiction to translational control via 4EBP-eIF4E.

Cancer cell

Hsieh AC, Costa M, Zollo O, Davis C, Feldman ME, Testa JR, Meyuhas O, Shokat KM, Ruggero D

Chemical genetic approach for kinase-substrate mapping by covalent capture of thiophosphopeptides and analysis by mass spectrometry.

Current protocols in chemical biology

Hertz NT, Wang BT, Allen JJ, Zhang C, Dar AC, Burlingame AL, Shokat KM

Mutant Ikzf1, KrasG12D, and Notch1 cooperate in T lineage leukemogenesis and modulate responses to targeted agents.

Proceedings of the National Academy of Sciences of the United States of America

Dail M, Li Q, McDaniel A, Wong J, Akagi K, Huang B, Kang HC, Kogan SC, Shokat K, Wolff L, Braun BS, Shannon K

The p110delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors.

Nature chemical biology

Berndt A, Miller S, Williams O, Le DD, Houseman BT, Pacold JI, Gorrec F, Hon WC, Liu Y, Rommel C, Gaillard P, Rückle T, Schwarz MK, Shokat KM, Shaw JP, Williams RL

Discovery of dual inhibitors of the immune cell PI3Ks p110delta and p110gamma: a prototype for new anti-inflammatory drugs.

Chemistry & biology

Williams O, Houseman BT, Kunkel EJ, Aizenstein B, Hoffman R, Knight ZA, Shokat KM

Dynamic regulation of a metabolic multi-enzyme complex by protein kinase CK2.

The Journal of biological chemistry

An S, Kyoung M, Allen JJ, Shokat KM, Benkovic SJ

Targeting the cancer kinome through polypharmacology.

Nature reviews. Cancer

Knight ZA, Lin H, Shokat KM

The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors.

Nature chemical biology

Berndt A, Miller S, Williams O, Le DD, Houseman BT, Pacold JI, Gorrec F, Hon WC, Liu Y, Rommel C, Gaillard P, Rückle T, Schwarz MK, Shokat KM, Shaw JP, Williams RL

Resiliency and vulnerability in the HER2-HER3 tumorigenic driver.

Science translational medicine

Amin DN, Sergina N, Ahuja D, McMahon M, Blair JA, Wang D, Hann B, Koch KM, Shokat KM, Moasser MM

New inhibitors of the PI3K-Akt-mTOR pathway: insights into mTOR signaling from a new generation of Tor Kinase Domain Inhibitors (TORKinibs).

Current topics in microbiology and immunology

Feldman ME, Shokat KM

Transforming growth factor beta1 inhibits cystic fibrosis transmembrane conductance regulator-dependent cAMP-stimulated alveolar epithelial fluid transport via a phosphatidylinositol 3-kinase-dependent mechanism.

The Journal of biological chemistry

Roux J, Carles M, Koh H, Goolaerts A, Ganter MT, Chesebro BB, Howard M, Houseman BT, Finkbeiner W, Shokat KM, Paquet AC, Matthay MA, Pittet JF

Regulation of meiotic recombination via Mek1-mediated Rad54 phosphorylation.

Molecular cell

Niu H, Wan L, Busygina V, Kwon Y, Allen JA, Li X, Kunz RC, Kubota K, Wang B, Sung P, Shokat KM, Gygi SP, Hollingsworth NM

Arterial-venous segregation by selective cell sprouting: an alternative mode of blood vessel formation.

Science (New York, N.Y.)

Herbert SP, Huisken J, Kim TN, Feldman ME, Houseman BT, Wang RA, Shokat KM, Stainier DY

Use of a semisynthetic epitope to probe histidine kinase activity and regulation.

Analytical biochemistry

Carlson HK, Plate L, Price MS, Allen JJ, Shokat KM, Marletta MA

Identifying genotype-dependent efficacy of single and combined PI3K- and MAPK-pathway inhibition in cancer.

Proceedings of the National Academy of Sciences of the United States of America

Sos ML, Fischer S, Ullrich R, Peifer M, Heuckmann JM, Koker M, Heynck S, Stückrath I, Weiss J, Fischer F, Michel K, Goel A, Regales L, Politi KA, Perera S, Getlik M, Heukamp LC, Ansén S, Zander T, Beroukhim R, Kashkar H, Shokat KM, Sellers WR, Rauh D, Orr C, Hoeflich KP, Friedman L, Wong KK, Pao W, Thomas RK

TFIIH-associated Cdk7 kinase functions in phosphorylation of C-terminal domain Ser7 residues, promoter-proximal pausing, and termination by RNA polymerase II.

Molecular and Cellular Biology

Glover-Cutter K, Larochelle S, Erickson B, Zhang C, Shokat K, Fisher RP, Bentley DL

Phosphorylation of the transcription elongation factor Spt5 by yeast Bur1 kinase stimulates recruitment of the PAF complex.

Molecular and Cellular Biology

Liu Y, Warfield L, Zhang C, Luo J, Allen J, Lang WH, Ranish J, Shokat KM, Hahn S

PIKfyve regulation of endosome-linked pathways.

Traffic (Copenhagen, Denmark)

de Lartigue J, Polson H, Feldman M, Shokat K, Tooze SA, Urbé S, Clague MJ

Evolution of phosphoregulation: comparison of phosphorylation patterns across yeast species.

PLoS biology

Beltrao P, Trinidad JC, Fiedler D, Roguev A, Lim WA, Shokat KM, Burlingame AL, Krogan NJ

Inhibitor hijacking of Akt activation.

Nature chemical biology

Okuzumi T, Fiedler D, Zhang C, Gray DC, Aizenstein B, Hoffman R, Shokat KM

Plk1 self-organization and priming phosphorylation of HsCYK-4 at the spindle midzone regulate the onset of division in human cells.

PLoS biology

Burkard ME, Maciejowski J, Rodriguez-Bravo V, Repka M, Lowery DM, Clauser KR, Zhang C, Shokat KM, Carr SA, Yaffe MB, Jallepalli PV

Tuning the activation threshold of a kinase network by nested feedback loops.

Science (New York, N.Y.)

Justman QA, Serber Z, Ferrell JE, El-Samad H, Shokat KM

Bypassing kinase activity of the tomato Pto resistance protein with small molecule ligands.

The Journal of biological chemistry

Salomon D, Bonshtien A, Mayrose M, Zhang C, Shokat KM, Sessa G

TFIIH and P-TEFb coordinate transcription with capping enzyme recruitment at specific genes in fission yeast.

Molecular cell

Viladevall L, St Amour CV, Rosebrock A, Schneider S, Zhang C, Allen JJ, Shokat KM, Schwer B, Leatherwood JK, Fisher RP

Isoform-selective phosphoinositide 3'-kinase inhibitors inhibit CXCR4 signaling and overcome stromal cell-mediated drug resistance in chronic lymphocytic leukemia: a novel therapeutic approach.

Blood

Niedermeier M, Hennessy BT, Knight ZA, Henneberg M, Hu J, Kurtova AV, Wierda WG, Keating MJ, Shokat KM, Burger JA

Phosphorylation of the SRC epithelial substrate Trask is tightly regulated in normal epithelia but widespread in many human epithelial cancers.

Clinical cancer research : an official journal of the American Association for Cancer Research

Wong CH, Baehner FL, Spassov DS, Ahuja D, Wang D, Hann B, Blair J, Shokat K, Welm AL, Moasser MM

Functional organization of the S. cerevisiae phosphorylation network.

Cell

Fiedler D, Braberg H, Mehta M, Chechik G, Cagney G, Mukherjee P, Silva AC, Shales M, Collins SR, van Wageningen S, Kemmeren P, Holstege FC, Weissman JS, Keogh MC, Koller D, Shokat KM, Krogan NJ

Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2.

PLoS biology

Feldman ME, Apsel B, Uotila A, Loewith R, Knight ZA, Ruggero D, Shokat KM

A complex-based reconstruction of the Saccharomyces cerevisiae interactome.

Molecular & cellular proteomics : MCP

Wang H, Kakaradov B, Collins SR, Karotki L, Fiedler D, Shales M, Shokat KM, Walther TC, Krogan NJ, Koller D

EGFR signals to mTOR through PKC and independently of Akt in glioma.

Science signaling

Fan QW, Cheng C, Knight ZA, Haas-Kogan D, Stokoe D, James CD, McCormick F, Shokat KM, Weiss WA

Basal subtype and MAPK/ERK kinase (MEK)-phosphoinositide 3-kinase feedback signaling determine susceptibility of breast cancer cells to MEK inhibition.

Cancer research

Mirzoeva OK, Das D, Heiser LM, Bhattacharya S, Siwak D, Gendelman R, Bayani N, Wang NJ, Neve RM, Guan Y, Hu Z, Knight Z, Feiler HS, Gascard P, Parvin B, Spellman PT, Shokat KM, Wyrobek AJ, Bissell MJ, McCormick F, Kuo WL, Mills GB, Gray JW, Korn WM

Generation of a novel system for studying spleen tyrosine kinase function in macrophages and B cells.

Journal of immunology (Baltimore, Md. : 1950)

Miller AL, Zhang C, Shokat KM, Lowell CA

SHIP prevents lipopolysaccharide from triggering an antiviral response in mice.

Blood

Sly LM, Hamilton MJ, Kuroda E, Ho VW, Antignano FL, Omeis SL, van Netten-Thomas CJ, Wong D, Brugger HK, Williams O, Feldman ME, Houseman BT, Fiedler D, Shokat KM, Krystal G

Cdk1-dependent phosphorylation of Cdc13 coordinates telomere elongation during cell-cycle progression.

Cell

Li S, Makovets S, Matsuguchi T, Blethrow JD, Shokat KM, Blackburn EH

Tuning a three-component reaction for trapping kinase substrate complexes.

Journal of the American Chemical Society

Statsuk AV, Maly DJ, Seeliger MA, Fabian MA, Biggs WH, Lockhart DJ, Zarrinkar PP, Kuriyan J, Shokat KM

The unfolded protein response signals through high-order assembly of Ire1.

Nature

Korennykh AV, Egea PF, Korostelev AA, Finer-Moore J, Zhang C, Shokat KM, Stroud RM, Walter P

Tissue-specific PKA inhibition using a chemical genetic approach and its application to studies on sperm capacitation.

Proceedings of the National Academy of Sciences of the United States of America

Morgan DJ, Weisenhaus M, Shum S, Su T, Zheng R, Zhang C, Shokat KM, Hille B, Babcock DF, McKnight GS

Distinct activation pathways confer cyclin-binding specificity on Cdk1 and Cdk2 in human cells.

Molecular cell

Merrick KA, Larochelle S, Zhang C, Allen JJ, Shokat KM, Fisher RP

Distinct roles of class IA PI3K isoforms in primary and immortalised macrophages.

Journal of cell science

Papakonstanti EA, Zwaenepoel O, Bilancio A, Burns E, Nock GE, Houseman B, Shokat K, Ridley AJ, Vanhaesebroeck B

Protein kinase Cdelta regulates ethanol intoxication and enhancement of GABA-stimulated tonic current.

The Journal of neuroscience : the official journal of the Society for Neuroscience

Choi DS, Wei W, Deitchman JK, Kharazia VN, Lesscher HM, McMahon T, Wang D, Qi ZH, Sieghart W, Zhang C, Shokat KM, Mody I, Messing RO

Structure and substrate recruitment of the human spindle checkpoint kinase Bub1.

Molecular cell

Kang J, Yang M, Li B, Qi W, Zhang C, Shokat KM, Tomchick DR, Machius M, Yu H

A chemical genomics study identifies Snf1 as a repressor of GCN4 translation.

The Journal of biological chemistry

Shirra MK, McCartney RR, Zhang C, Shokat KM, Schmidt MC, Arndt KM

Small molecule recognition of c-Src via the Imatinib-binding conformation.

Chemistry & biology

Dar AC, Lopez MS, Shokat KM

Dual inhibition of PI3Kalpha and mTOR as an alternative treatment for Kaposi's sarcoma.

Cancer research

Chaisuparat R, Hu J, Jham BC, Knight ZA, Shokat KM, Montaner S

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.

Nature chemical biology

Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA

The yeast LATS/Ndr kinase Cbk1 regulates growth via Golgi-dependent glycosylation and secretion.

Molecular biology of the cell

Kurischko C, Kuravi VK, Wannissorn N, Nazarov PA, Husain M, Zhang C, Shokat KM, McCaffery JM, Luca FC

A chemical screen in diverse breast cancer cell lines reveals genetic enhancers and suppressors of sensitivity to PI3K isoform-selective inhibition.

The Biochemical journal

Torbett NE, Luna-Moran A, Knight ZA, Houk A, Moasser M, Weiss W, Shokat KM, Stokoe D

Genetic or pharmaceutical blockade of p110delta phosphoinositide 3-kinase enhances IgE production.

The Journal of allergy and clinical immunology

Zhang TT, Okkenhaug K, Nashed BF, Puri KD, Knight ZA, Shokat KM, Vanhaesebroeck B, Marshall AJ

PIK3CA cooperates with other phosphatidylinositol 3'-kinase pathway mutations to effect oncogenic transformation.

Cancer research

Oda K, Okada J, Timmerman L, Rodriguez-Viciana P, Stokoe D, Shoji K, Taketani Y, Kuramoto H, Knight ZA, Shokat KM, McCormick F

Human carbonyl reductase 1 is an S-nitrosoglutathione reductase.

The Journal of biological chemistry

Bateman RL, Rauh D, Tavshanjian B, Shokat KM

A chemical-genetic strategy reveals distinct temporal requirements for SAD-1 kinase in neuronal polarization and synapse formation.

Neural development

Kim JS, Lilley BN, Zhang C, Shokat KM, Sanes JR, Zhen M

The effect of H3K79 dimethylation and H4K20 trimethylation on nucleosome and chromatin structure.

Nature structural & molecular biology

Lu X, Simon MD, Chodaparambil JV, Hansen JC, Shokat KM, Luger K

Ablation of PI3K blocks BCR-ABL leukemogenesis in mice, and a dual PI3K/mTOR inhibitor prevents expansion of human BCR-ABL+ leukemia cells.

The Journal of clinical investigation

Kharas MG, Janes MR, Scarfone VM, Lilly MB, Knight ZA, Shokat KM, Fruman DA

Discovery of drug-resistant and drug-sensitizing mutations in the oncogenic PI3K isoform p110 alpha.

Cancer cell

Zunder ER, Knight ZA, Houseman BT, Apsel B, Shokat KM

The brain-derived neurotrophic factor receptor TrkB is critical for the acquisition but not expression of conditioned incentive value.

The European journal of neuroscience

Johnson AW, Chen X, Crombag HS, Zhang C, Smith DR, Shokat KM, Gallagher M, Holland PC, Ginty DD

Activity of the p110-alpha subunit of phosphatidylinositol-3-kinase is required for activation of epithelial sodium transport.

American journal of physiology. Renal physiology

Wang J, Knight ZA, Fiedler D, Williams O, Shokat KM, Pearce D

An integrated platform of genomic assays reveals small-molecule bioactivities.

Nature chemical biology

Hoon S, Smith AM, Wallace IM, Suresh S, Miranda M, Fung E, Proctor M, Shokat KM, Zhang C, Davis RW, Giaever G, St Onge RP, StOnge RP, Nislow C

Nuclear HuR accumulation through phosphorylation by Cdk1.

Genes & development

Kim HH, Abdelmohsen K, Lal A, Pullmann R, Yang X, Galban S, Srikantan S, Martindale JL, Blethrow J, Shokat KM, Gorospe M

Hyperphosphorylation of RNA polymerase II in response to topoisomerase I cleavage complexes and its association with transcription- and BRCA1-dependent degradation of topoisomerase I.

Journal of molecular biology

Sordet O, Larochelle S, Nicolas E, Stevens EV, Zhang C, Shokat KM, Fisher RP, Pommier Y

PI-103, a dual inhibitor of Class IA phosphatidylinositide 3-kinase and mTOR, has antileukemic activity in AML.

Leukemia

Park S, Chapuis N, Bardet V, Tamburini J, Gallay N, Willems L, Knight ZA, Shokat KM, Azar N, Viguié F, Ifrah N, Dreyfus F, Mayeux P, Lacombe C, Bouscary D

T cell receptor signaling controls Foxp3 expression via PI3K, Akt, and mTOR.

Proceedings of the National Academy of Sciences of the United States of America

Sauer S, Bruno L, Hertweck A, Finlay D, Leleu M, Spivakov M, Knight ZA, Cobb BS, Cantrell D, O'Connor E, Shokat KM, Fisher AG, Merkenschlager M

Analysis of 3-phosphoinositide-dependent kinase-1 signaling and function in ES cells.

Experimental cell research

Tamgüney T, Zhang C, Fiedler D, Shokat K, Stokoe D

Characterization of structurally distinct, isoform-selective phosphoinositide 3'-kinase inhibitors in combination with radiation in the treatment of glioblastoma.

Molecular cancer therapeutics

Chen JS, Zhou LJ, Entin-Meer M, Yang X, Donker M, Knight ZA, Weiss W, Shokat KM, Haas-Kogan D, Stokoe D

Inhibition of ZAP-70 kinase activity via an analog-sensitive allele blocks T cell receptor and CD28 superagonist signaling.

The Journal of biological chemistry

Levin SE, Zhang C, Kadlecek TA, Shokat KM, Weiss A

Cdc28-Clb5 (CDK-S) and Cdc7-Dbf4 (DDK) collaborate to initiate meiotic recombination in yeast.

Genes & development

Wan L, Niu H, Futcher B, Zhang C, Shokat KM, Boulton SJ, Hollingsworth NM

Covalent capture of kinase-specific phosphopeptides reveals Cdk1-cyclin B substrates.

Proceedings of the National Academy of Sciences of the United States of America

Blethrow JD, Glavy JS, Morgan DO, Shokat KM

Design of drug-resistant alleles of type-III phosphatidylinositol 4-kinases using mutagenesis and molecular modeling.

Biochemistry

Balla A, Tuymetova G, Toth B, Szentpetery Z, Zhao X, Knight ZA, Shokat K, Steinbach PJ, Balla T

Maintenance of hormone-sensitive phosphoinositide pools in the plasma membrane requires phosphatidylinositol 4-kinase IIIalpha.

Molecular biology of the cell

Balla A, Kim YJ, Varnai P, Szentpetery Z, Knight Z, Shokat KM, Balla T

Recognizing and exploiting differences between RNAi and small-molecule inhibitors.

Nature chemical biology

Weiss WA, Taylor SS, Shokat KM

IRE1 signaling affects cell fate during the unfolded protein response.

Science (New York, N.Y.)

Lin JH, Li H, Yasumura D, Cohen HR, Zhang C, Panning B, Shokat KM, Lavail MM, Walter P

Access denied: Snf1 activation loop phosphorylation is controlled by availability of the phosphorylated threonine 210 to the PP1 phosphatase.

The Journal of biological chemistry

Rubenstein EM, McCartney RR, Zhang C, Shokat KM, Shirra MK, Arndt KM, Schmidt MC

A coupled chemical-genetic and bioinformatic approach to Polo-like kinase pathway exploration.

Chemistry & biology

Snead JL, Sullivan M, Lowery DM, Cohen MS, Zhang C, Randle DH, Taunton J, Yaffe MB, Morgan DO, Shokat KM

A surface on the androgen receptor that allosterically regulates coactivator binding.

Proceedings of the National Academy of Sciences of the United States of America

Estébanez-Perpiñá E, Arnold LA, Arnold AA, Nguyen P, Rodrigues ED, Mar E, Bateman R, Pallai P, Shokat KM, Baxter JD, Guy RK, Webb P, Fletterick RJ

Suppression of p53-dependent senescence by the JNK signal transduction pathway.

Proceedings of the National Academy of Sciences of the United States of America

Das M, Jiang F, Sluss HK, Zhang C, Shokat KM, Flavell RA, Davis RJ

Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits.

The Journal of biological chemistry

Qi ZH, Song M, Wallace MJ, Wang D, Newton PM, McMahon T, Chou WH, Zhang C, Shokat KM, Messing RO

A remodelled protease that cleaves phosphotyrosine substrates.

Journal of the American Chemical Society

Knight ZA, Garrison JL, Chan K, King DS, Shokat KM

A dual phosphoinositide-3-kinase alpha/mTOR inhibitor cooperates with blockade of epidermal growth factor receptor in PTEN-mutant glioma.

Cancer research

Fan QW, Cheng CK, Nicolaides TP, Hackett CS, Knight ZA, Shokat KM, Weiss WA

Glutathione traps formaldehyde by formation of a bicyclo[4.4.1]undecane adduct.

Organic & biomolecular chemistry

Bateman R, Rauh D, Shokat KM

A semisynthetic epitope for kinase substrates.

Nature methods

Allen JJ, Li M, Brinkworth CS, Paulson JL, Wang D, Hübner A, Chou WH, Davis RJ, Burlingame AL, Messing RO, Katayama CD, Hedrick SM, Shokat KM

HIV-1 Nef assembles a Src family kinase-ZAP-70/Syk-PI3K cascade to downregulate cell-surface MHC-I.

Cell host & microbe

Hung CH, Thomas L, Ruby CE, Atkins KM, Morris NP, Knight ZA, Scholz I, Barklis E, Weinberg AD, Shokat KM, Thomas G

Chemically targeting the PI3K family.

Biochemical Society transactions

Knight ZA, Shokat KM

Chemical inhibition of the TFIIH-associated kinase Cdk7/Kin28 does not impair global mRNA synthesis.

Proceedings of the National Academy of Sciences of the United States of America

Kanin EI, Kipp RT, Kung C, Slattery M, Viale A, Hahn S, Shokat KM, Ansari AZ

Requirements for Cdk7 in the assembly of Cdk1/cyclin B and activation of Cdk2 revealed by chemical genetics in human cells.

Molecular cell

Larochelle S, Merrick KA, Terret ME, Wohlbold L, Barboza NM, Zhang C, Shokat KM, Jallepalli PV, Fisher RP

The site-specific installation of methyl-lysine analogs into recombinant histones.

Cell

Simon MD, Chu F, Racki LR, de la Cruz CC, Burlingame AL, Panning B, Narlikar GJ, Shokat KM

Chemical genetics reveals the requirement for Polo-like kinase 1 activity in positioning RhoA and triggering cytokinesis in human cells.

Proceedings of the National Academy of Sciences of the United States of America

Burkard ME, Randall CL, Larochelle S, Zhang C, Shokat KM, Fisher RP, Jallepalli PV

Structure-guided development of affinity probes for tyrosine kinases using chemical genetics.

Nature chemical biology

Blair JA, Rauh D, Kung C, Yun CH, Fan QW, Rode H, Zhang C, Eck MJ, Weiss WA, Shokat KM

Chemical genetics: where genetics and pharmacology meet.

Cell

Knight ZA, Shokat KM

Escape from HER-family tyrosine kinase inhibitor therapy by the kinase-inactive HER3.

Nature

Sergina NV, Rausch M, Wang D, Blair J, Hann B, Shokat KM, Moasser MM

A membrane capture assay for lipid kinase activity.

Nature protocols

Knight ZA, Feldman ME, Balla A, Balla T, Shokat KM

Construction of conditional analog-sensitive kinase alleles in the fission yeast Schizosaccharomyces pombe.

Nature protocols

Gregan J, Zhang C, Rumpf C, Cipak L, Li Z, Uluocak P, Nasmyth K, Shokat KM

Structure and properties of a re-engineered homeodomain protein-DNA interface.

ACS chemical biology

Simon MD, Feldman ME, Rauh D, Maris AE, Wemmer DE, Shokat KM

Chemical inactivation of cdc7 kinase in budding yeast results in a reversible arrest that allows efficient cell synchronization prior to meiotic recombination.

Genetics

Wan L, Zhang C, Shokat KM, Hollingsworth NM

Phosphatidylinositol 4-kinase IIIbeta regulates the transport of ceramide between the endoplasmic reticulum and Golgi.

The Journal of biological chemistry

Tóth B, Balla A, Ma H, Knight ZA, Shokat KM, Balla T

JNK2 is a positive regulator of the cJun transcription factor.

Molecular cell

Jaeschke A, Karasarides M, Ventura JJ, Ehrhardt A, Zhang C, Flavell RA, Shokat KM, Davis RJ

To stabilize neutrophil polarity, PIP3 and Cdc42 augment RhoA activity at the back as well as signals at the front.

The Journal of Cell Biology

Van Keymeulen A, Wong K, Knight ZA, Govaerts C, Hahn KM, Shokat KM, Bourne HR

Arabidopsis MAP kinase 4 regulates salicylic acid- and jasmonic acid/ethylene-dependent responses via EDS1 and PAD4.

The Plant journal : for cell and molecular biology

Brodersen P, Petersen M, Bjørn Nielsen H, Zhu S, Newman MA, Shokat KM, Rietz S, Parker J, Mundy J

Forebrain overexpression of CaMKII abolishes cingulate long term depression and reduces mechanical allodynia and thermal hyperalgesia.

Molecular pain

Wei F, Wang GD, Zhang C, Shokat KM, Wang H, Tsien JZ, Liauw J, Zhuo M

A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma.

Cancer cell

Fan QW, Knight ZA, Goldenberg DD, Yu W, Mostov KE, Stokoe D, Shokat KM, Weiss WA

A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling.

Cell

Knight ZA, Gonzalez B, Feldman ME, Zunder ER, Goldenberg DD, Williams O, Loewith R, Stokoe D, Balla A, Toth B, Balla T, Weiss WA, Williams RL, Shokat KM

Chemical genomics: dialed in transcriptional network control with non-steroidal glucocorticoid receptor modulators.

ACS chemical biology

Allen JJ, Shokat KM

Effect of combined DNA repair inhibition and G2 checkpoint inhibition on cell cycle progression after DNA damage.

Molecular cancer therapeutics

Sturgeon CM, Knight ZA, Shokat KM, Roberge M

Selective kinase inhibition by exploiting differential pathway sensitivity.

Chemistry & biology

Kung C, Kenski DM, Krukenberg K, Madhani HD, Shokat KM

Chemical genetic analysis of the time course of signal transduction by JNK.

Molecular cell

Ventura JJ, Hübner A, Zhang C, Flavell RA, Shokat KM, Davis RJ

The cyclin-dependent kinase (CDK) family member PNQALRE/CCRK supports cell proliferation but has no intrinsic CDK-activating kinase (CAK) activity.

Cell cycle (Georgetown, Tex.)

Wohlbold L, Larochelle S, Liao JC, Livshits G, Singer J, Shokat KM, Fisher RP

Identification of otubain 1 as a novel substrate for the Yersinia protein kinase using chemical genetics and mass spectrometry.

FEBS letters

Juris SJ, Shah K, Shokat K, Dixon JE, Vacratsis PO

Combining chemical genetics and proteomics to identify protein kinase substrates.

Proceedings of the National Academy of Sciences of the United States of America

Dephoure N, Howson RW, Blethrow JD, Shokat KM, O'Shea EK

Dichotomous but stringent substrate selection by the dual-function Cdk7 complex revealed by chemical genetics.

Nature structural & molecular biology

Larochelle S, Batliner J, Gamble MJ, Barboza NM, Kraybill BC, Blethrow JD, Shokat KM, Fisher RP

The Ipl1-Aurora protein kinase activates the spindle checkpoint by creating unattached kinetochores.

Nature cell biology

Pinsky BA, Kung C, Shokat KM, Biggins S

Chemical genetic engineering of G protein-coupled receptor kinase 2.

The Journal of biological chemistry

Kenski DM, Zhang C, von Zastrow M, Shokat KM

The protein kinase Kin4 inhibits exit from mitosis in response to spindle position defects.

Molecular cell

D'Aquino KE, Monje-Casas F, Paulson J, Reiser V, Charles GM, Lai L, Shokat KM, Amon A

A second-site suppressor strategy for chemical genetic analysis of diverse protein kinases.

Nature methods

Zhang C, Kenski DM, Paulson JL, Bonshtien A, Sessa G, Cross JV, Templeton DJ, Shokat KM

Features of selective kinase inhibitors.

Chemistry & biology

Knight ZA, Shokat KM

Structural bioinformatics-based design of selective, irreversible kinase inhibitors.

Science (New York, N.Y.)

Cohen MS, Zhang C, Shokat KM, Taunton J

Chemicals call bacteria, and a new membrane protein machine answers.

Cell

Shokat KM

Bio-orthogonal affinity purification of direct kinase substrates.

Journal of the American Chemical Society

Allen JJ, Lazerwith SE, Shokat KM

Targeting the gatekeeper residue in phosphoinositide 3-kinases.

Bioorganic & medicinal chemistry

Alaimo PJ, Knight ZA, Shokat KM

A chemical-genetic approach to studying neurotrophin signaling.

Neuron

Chen X, Ye H, Kuruvilla R, Ramanan N, Scangos KW, Zhang C, Johnson NM, England PM, Shokat KM, Ginty DD

An unbiased cell morphology-based screen for new, biologically active small molecules.

PLoS biology

Tanaka M, Bateman R, Rauh D, Vaisberg E, Ramachandani S, Zhang C, Hansen KC, Burlingame AL, Trautman JK, Shokat KM, Adams CL

The F box protein Dsg1/Mdm30 is a transcriptional coactivator that stimulates Gal4 turnover and cotranscriptional mRNA processing.

Cell

Muratani M, Kung C, Shokat KM, Tansey WP

Small-molecule kinase-inhibitor target assessment.

Chembiochem : a European journal of chemical biology

Kung C, Shokat KM

Chemical genomic profiling to identify intracellular targets of a multiplex kinase inhibitor.

Proceedings of the National Academy of Sciences of the United States of America

Kung C, Kenski DM, Dickerson SH, Howson RW, Kuyper LF, Madhani HD, Shokat KM

Chemical genetics reveals a role for Mps1 kinase in kinetochore attachment during mitosis.

Current biology : CB

Jones MH, Huneycutt BJ, Pearson CG, Zhang C, Morgan G, Shokat K, Bloom K, Winey M

Sole BCR-ABL inhibition is insufficient to eliminate all myeloproliferative disorder cell populations.

Proceedings of the National Academy of Sciences of the United States of America

Wong S, McLaughlin J, Cheng D, Zhang C, Shokat KM, Witte ON

Isoform-specific phosphoinositide 3-kinase inhibitors from an arylmorpholine scaffold.

Bioorganic & medicinal chemistry

Knight ZA, Chiang GG, Alaimo PJ, Kenski DM, Ho CB, Coan K, Abraham RT, Shokat KM

A mechanism-based cross-linker for the identification of kinase-substrate pairs.

Journal of the American Chemical Society

Maly DJ, Allen JA, Shokat KM

Rapid structure-activity and selectivity analysis of kinase inhibitors by BioMAP analysis in complex human primary cell-based models.

Assay and drug development technologies

Kunkel EJ, Plavec I, Nguyen D, Melrose J, Rosler ES, Kao LT, Wang Y, Hytopoulos E, Bishop AC, Bateman R, Shokat KM, Butcher EC, Berg EL

A phage display selection of engrailed homeodomain mutants and the importance of residue Q50.

Nucleic Acids Research

Simon MD, Sato K, Weiss GA, Shokat KM

Adaptability at a protein-DNA interface: re-engineering the engrailed homeodomain to recognize an unnatural nucleotide.

Journal of the American Chemical Society

Simon MD, Shokat KM

Dissecting the Engrailed homeodomain-DNA interaction by phage-displayed shotgun scanning.

Chemistry & biology

Sato K, Simon MD, Levin AM, Shokat KM, Weiss GA

Design and use of analog-sensitive protein kinases.

Current protocols in molecular biology

Blethrow J, Zhang C, Shokat KM, Weiss EL

Chemical-genetic inhibition of a sensitized mutant myosin Vb demonstrates a role in peripheral-pericentriolar membrane traffic.

Proceedings of the National Academy of Sciences of the United States of America

Provance DW, Gourley CR, Silan CM, Cameron LC, Shokat KM, Goldenring JR, Shah K, Gillespie PG, Mercer JA

Two cyclin-dependent kinases promote RNA polymerase II transcription and formation of the scaffold complex.

Molecular and Cellular Biology

Liu Y, Kung C, Fishburn J, Ansari AZ, Shokat KM, Hahn S

Engineering the serine/threonine protein kinase Raf-1 to utilise an orthogonal analogue of ATP substituted at the N6 position.

FEBS letters

Hindley AD, Park S, Wang L, Shah K, Wang Y, Hu X, Shokat KM, Kolch W, Sedivy JM, Yeung KC

Combinatorial efficacy achieved through two-point blockade within a signaling pathway-a chemical genetic approach.

Cancer research

Fan QW, Specht KM, Zhang C, Goldenberg DD, Shokat KM, Weiss WA

Mek1 kinase activity functions downstream of RED1 in the regulation of meiotic double strand break repair in budding yeast.

Molecular biology of the cell

Wan L, de los Santos T, Zhang C, Shokat K, Hollingsworth NM

Targets of the cyclin-dependent kinase Cdk1.

Nature

Ubersax JA, Woodbury EL, Quang PN, Paraz M, Blethrow JD, Shah K, Shokat KM, Morgan DO

Bypassing a kinase activity with an ATP-competitive drug.

Science (New York, N.Y.)

Papa FR, Zhang C, Shokat K, Walter P

Dynamic phosphoregulation of the cortical actin cytoskeleton and endocytic machinery revealed by real-time chemical genetic analysis.

The Journal of Cell Biology

Sekiya-Kawasaki M, Groen AC, Cope MJ, Kaksonen M, Watson HA, Zhang C, Shokat KM, Wendland B, McDonald KL, McCaffery JM, Drubin DG

Specific inhibition of Elm1 kinase activity reveals functions required for early G1 events.

Molecular and Cellular Biology

Sreenivasan A, Bishop AC, Shokat KM, Kellogg DR

Phosphospecific proteolysis for mapping sites of protein phosphorylation.

Nature biotechnology

Knight ZA, Schilling B, Row RH, Kenski DM, Gibson BW, Shokat KM

Cutting edge: a chemical genetic system for the analysis of kinases regulating T cell development.

Journal of immunology (Baltimore, Md. : 1950)

Denzel A, Hare KJ, Zhang C, Shokat K, Jenkinson EJ, Anderson G, Hayday A

Engineering a "methionine clamp" into Src family kinases enhances specificity toward unnatural ATP analogues.

Biochemistry

Ulrich SM, Kenski DM, Shokat KM

Control of landmark events in meiosis by the CDK Cdc28 and the meiosis-specific kinase Ime2.

Genes & development

Benjamin KR, Zhang C, Shokat KM, Herskowitz I

Inducible protein knockout reveals temporal requirement of CaMKII reactivation for memory consolidation in the brain.

Proceedings of the National Academy of Sciences of the United States of America

Wang H, Shimizu E, Tang YP, Cho M, Kyin M, Zuo W, Robinson DA, Alaimo PJ, Zhang C, Morimoto H, Zhuo M, Feng R, Shokat KM, Tsien JZ

Identification of novel ERK2 substrates through use of an engineered kinase and ATP analogs.

The Journal of biological chemistry

Eblen ST, Kumar NV, Shah K, Henderson MJ, Watts CK, Shokat KM, Weber MJ

Chemical genetic analysis of Apg1 reveals a non-kinase role in the induction of autophagy.

Molecular biology of the cell

Abeliovich H, Zhang C, Dunn WA, Shokat KM, Klionsky DJ

A chemical genetic approach for the identification of direct substrates of protein kinases.

Methods in molecular biology (Clifton, N.J.)

Shah K, Shokat KM

Conformational restraint is a critical determinant of unnatural nucleotide recognition by protein kinases.

Bioorganic & medicinal chemistry letters

Ulrich SM, Sallee NA, Shokat KM

Inhibitor scaffolds as new allele specific kinase substrates.

Journal of the American Chemical Society

Kraybill BC, Elkin LL, Blethrow JD, Morgan DO, Shokat KM

A kinase sequence database: sequence alignments and family assignment.

Bioinformatics (Oxford, England)

Buzko O, Shokat KM

The Saccharomyces cerevisiae Mob2p-Cbk1p kinase complex promotes polarized growth and acts with the mitotic exit network to facilitate daughter cell-specific localization of Ace2p transcription factor.

The Journal of Cell Biology

Weiss EL, Kurischko C, Zhang C, Shokat K, Drubin DG, Luca FC

Chemical genetic blockade of transformation reveals dependence on aberrant oncogenic signaling.

Current biology : CB

Fan QW, Zhang C, Shokat KM, Weiss WA

Novel chemical genetic approaches to the discovery of signal transduction inhibitors.

Drug discovery today

Shokat K, Velleca M

Protein engineering of protein kinase A catalytic subunits results in the acquisition of novel inhibitor sensitivity.

The Journal of biological chemistry

Niswender CM, Ishihara RW, Judge LM, Zhang C, Shokat KM, McKnight GS

The emerging power of chemical genetics.

Current opinion in cell biology

Specht KM, Shokat KM

A chemical-genetic strategy implicates myosin-1c in adaptation by hair cells.

Cell

Holt JR, Gillespie SK, Provance DW, Shah K, Shokat KM, Corey DP, Mercer JA, Gillespie PG

Chemical Genetic Analysis of Protein Kinase Cascades.

TheScientificWorldJournal

Alaimo PJ, Shogren-Knaak MA, Shokat KM

Modified AutoDock for accurate docking of protein kinase inhibitors.

Journal of computer-aided molecular design

Buzko OV, Bishop AC, Shokat KM

A chemical genetic screen for direct v-Src substrates reveals ordered assembly of a retrograde signaling pathway.

Chemistry & biology

Shah K, Shokat KM

Green fluorescent protein-based protein kinase biosensor substrates.

Methods in molecular biology (Clifton, N.J.)

Ulrich S, Shokat K

Mutant tyrosine kinases with unnatural nucleotide specificity retain the structure and phospho-acceptor specificity of the wild-type enzyme.

Chemistry & biology

Witucki LA, Huang X, Shah K, Liu Y, Kyin S, Eck MJ, Shokat KM

Chemical inhibition of the Pho85 cyclin-dependent kinase reveals a role in the environmental stress response.

Proceedings of the National Academy of Sciences of the United States of America

Carroll AS, Bishop AC, DeRisi JL, Shokat KM, O'Shea EK

Chemical genetic approaches for the elucidation of signaling pathways.

Current opinion in chemical biology

Alaimo PJ, Shogren-Knaak MA, Shokat KM

The LuxS family of bacterial autoinducers: biosynthesis of a novel quorum-sensing signal molecule.

Molecular microbiology

Schauder S, Shokat K, Surette MG, Bassler BL

Magic bullets for protein kinases.

Trends in cell biology

Bishop AC, Buzko O, Shokat KM

Identification of new JNK substrate using ATP pocket mutant JNK and a corresponding ATP analogue.

The Journal of biological chemistry

Habelhah H, Shah K, Huang L, Burlingame AL, Shokat KM, Ronai Z

ERK phosphorylation drives cytoplasmic accumulation of hnRNP-K and inhibition of mRNA translation.

Nature cell biology

Habelhah H, Shah K, Huang L, Ostareck-Lederer A, Burlingame AL, Shokat KM, Hentze MW, Ronai Z

Phage-display evolution of tyrosine kinases with altered nucleotide specificity.

Biopolymers

Ting AY, Witte K, Shah K, Kraybill B, Shokat KM, Schultz PG

Recent advances in chemical approaches to the study of biological systems.

Annual review of cell and developmental biology

Shogren-Knaak MA, Alaimo PJ, Shokat KM

Src-Abl tyrosine kinase chimeras: replacement of the adenine binding pocket of c-Abl with v-Src to swap nucleotide and inhibitor specificities.

Biochemistry

Liu Y, Witucki LA, Shah K, Bishop AC, Shokat KM

Engineering unnatural nucleotide specificity for Rous sarcoma virus tyrosine kinase to uniquely label its direct substrates.

Proceedings of the National Academy of Sciences of the United States of America

Shah K, Liu Y, Deirmengian C, Shokat KM

Immunoglobulin signal transduction guides the specificity of B cell-T cell interactions and is blocked in tolerant self-reactive B cells.

The Journal of experimental medicine

Cooke MP, Heath AW, Shokat KM, Zeng Y, Finkelman FD, Linsley PS, Howard M, Goodnow CC

Does the bifunctional uridylate synthase channel orotidine 5'-phosphate? Kinetics of orotate phosphoribosyltransferase and orotidylate decarboxylase activities fit a noninteracting sites model.

Biochemistry

McClard RW, Shokat KM

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Kevan Shokat, PhD