KCGS, PKIS2, and PKIS Publications

2018

Platzer C, Najjar A, Rhoe A, Erdmann F, Sippl W, Schmidt M. Identification of PKMYT1 inhibitors by screening the GSK published protein kinase inhibitor set I and II. Bioorg Med Chem. 2018 Jun 20. pii: S0968-0896(18)30496-6. doi: 10.1016/j.bmc.2018.06.027. [Epub ahead of print] PMID: 29941193

Byrne DP, Li Y, Ramakrishnan K, Barsukov IL, Yates EA, Eyers CE, Papy-Garcia D, Chantepie S, Pagadala V, Lu J, Wells C, Drewry DH, Zuercher WJ, Berry NG, Fernig DG, Eyers PA.. New tools for carbohydrate sulphation analysis: Heparan Sulphate 2- O -sulphotransferase (HS2ST) is a target for small molecule protein kinase inhibitors. Biochem J. 2018 Jun 22. pii: BCJ20180265. doi: 10.1042/BCJ20180265. [Epub ahead of print] PMID: 29934491

Byrne DP, Li Y, Ngamlert P, Ramakrishnan K, Eyers CE, Wells C, Drewry DH, Zuercher WJ, Berry NG, Fernig DG, Eyers PA. New tools for evaluating protein tyrosine sulphation: Tyrosyl Protein Sulphotransferases (TPSTs) are novel targets for RAF protein kinase inhibitors. Biochem J. 2018 Jun 22. pii: BCJ20180266. doi: 10.1042/BCJ20180266. [Epub ahead of print] PMID: 29934490

Krulikas LJ, McDonald IM, Lee B, Okumu DO, East MP, Gilbert TSK, Herring LE, Golitz BT, Wells CI, Axtman AD, Zuercher WJ, Willson TM, Kireev D, Yeh JJ, Johnson GL, Baines AT, Graves LM. Application of Integrated Drug Screening/Kinome Analysis to Identify Inhibitors of Gemcitabine-Resistant Pancreatic Cancer Cell Growth. SLAS Discov. 2018 May 1:2472555218773045. doi: 10.1177/2472555218773045. [Epub ahead of print]
PMID: 29742358

van Buggenum JAG, Gerlach JP, Tanis SEJ, Hogeweg M, Jansen PWTC, Middelwijk J, van der Steen R, Vermeulen M, Stunnenberg HG, Albers CA, Mulder KW.. Immuno-detection by sequencing enables large-scale high-dimensional phenotyping in cells. Nat Commun. 2018 Jun 19;9(1):2384. doi: 10.1038/s41467-018-04761-0. PMID: 29921844

2017

Hawkinson JE, Sinville R, Mudaliar D, Shetty J, Ward T, Herr JC, Georg GI. Potent Pyrimidine and Pyrrolopyrimidine Inhibitors of Testis-Specific Serine/Threonine Kinase 2 (TSSK2). ChemMedChem. 2017 Nov 22;12(22):1857-1865. doi: 10.1002/cmdc.201700503. Epub 2017 Oct 20. PMID: 28952188

Brägelmann J, Dammert MA, Dietlein F, Heuckmann JM, Choidas A, Böhm S, Richters A, Basu D, Tischler V, Lorenz C, Habenberger P, Fang Z, Ortiz-Cuaran S, Leenders F, Eickhoff J, Koch U, Getlik M, Termathe M, Sallouh M, Greff Z, Varga Z, Balke-Want H, French CA, Peifer M, Reinhardt HC, Örfi L, Kéri G, Ansén S, Heukamp LC, Büttner R, Rauh D, Klebl BM, Thomas RK, Sos ML. Systematic Kinase Inhibitor Profiling Identifies CDK9 as a Synthetic Lethal Target in NUT Midline Carcinoma. Cell Rep. 2017 Sep 19;20(12):2833-2845. doi: 10.1016/j.celrep.2017.08.082. PMID: 28930680

Williams CAC, Gray NS, Findlay GM. A Simple Method to Identify Kinases That Regulate Embryonic Stem Cell Pluripotency by High-throughput Inhibitor Screening.   J Vis Exp. 2017 May 12;(123). doi: 10.3791/55515.
PMID: 28570543

Cao J, Wang J, Jackman CP, Cox AH, Trembley MA, Balowski JJ, Cox BD, De Simone A, Dickson AL, Di Talia S, Small EM, Kiehart DP, Bursac N, Poss KD. Tension Creates an Endoreplication Wavefront that Leads Regeneration of Epicardial Tissue. Dev Cell. 2017 Sep 25;42(6):600-615.e4. doi: 10.1016/j.devcel.2017.08.024. PMID: 28950101

Piotrowski JS, Li SC, Deshpande R, Simpkins SW, Nelson J, Yashiroda Y, Barber JM, Safizadeh H, Wilson E, Okada H, Gebre AA, Kubo K, Torres NP, LeBlanc MA, Andrusiak K, Okamoto R, Yoshimura M, DeRango-Adem E, van Leeuwen J, Shirahige K, Baryshnikova A, Brown GW, Hirano H, Costanzo M, Andrews B, Ohya Y, Osada H, Yoshida M, Myers CL, Boone C. Functional annotation of chemical libraries across diverse biological processes. Nat Chem Biol. 2017 Sep;13(9):982-993. doi: 10.1038/nchembio.2436. Epub 2017 Jul 24.
Erratum in: Nat Chem Biol. 2017 Nov 21;13(12 ):1286. PMID: 28759014

Conant G, Ahadian S, Zhao Y, Radisic M. Kinase inhibitor screening using artificial neural networks and engineered cardiac biowires. Sci Rep. 2017 Sep 18;7(1):11807. doi: 10.1038/s41598-017-12048-5. PMID: 28924210

Mateus A, Gordon LJ, Wayne GJ, Almqvist H, Axelsson H, Seashore-Ludlow B, Treyer A, Matsson P, Lundbäck T, West A, Hann MM, Artursson P. Prediction of intracellular exposure bridges the gap between target- and cell-based drug discovery. Proc Natl Acad Sci U S A. 2017 Jul 25;114(30):E6231-E6239. doi: 10.1073/pnas.1701848114. Epub 2017 Jul 12. PMID: 28701380

Dixon-Clarke SE, Shehata SN, Krojer T, Sharpe TD, von Delft F, Sakamoto K, Bullock AN. Structure and inhibitor specificity of the PCTAIRE-family kinase CDK16. Biochem J. 2017 Feb 20;474(5):699-713. doi: 10.1042/BCJ20160941.
PMID: 28057719

Khan AS, Murray MJ, Ho CMK, Zuercher WJ, Reeves MB, Strang BL. High-throughput screening of a GlaxoSmithKline protein kinase inhibitor set identifies an inhibitor of human cytomegalovirus replication that prevents CREB and histone H3 post-translational modification. J Gen Virol. 2017 Apr;98(4):754-768. doi: 10.1099/jgv.0.000713. Epub 2017 Apr 20. PMID: 28100301

Schaenzer AJ, Wlodarchak N, Drewry DH, Zuercher WJ, Rose WE, Striker R, Sauer JD. A screen for kinase inhibitors identifies antimicrobial imidazopyridine aminofurazans as specific inhibitors of the Listeria monocytogenes PASTA kinase PrkA. J Biol Chem. 2017 Oct 13;292(41):17037-17045. doi: 10.1074/jbc.M117.808600. Epub 2017 Aug 16.
PMID: 28821610

Nathan Wlodarchak, Nathan Teachout, Rebecca Procknow, Jeff Beczkiewicz, Adam Schaenzer, Kenneth Satyshur, Martin Pavelka, Bill Zuercher, Dave Drewry, John-Demian Sauer, Rob Striker. Repurposed kinase inhibitors and beta-lactams as a novel therapy for antibiotic resistant bacteria. BioRxiv 199422 (2017)[preprint] doi: https://doi.org/10.1101/199422

Matossian MD, Elliott S, Hoang VT, Burks HE, Phamduy TB, Chrisey DB, Zuercher WJ, Drewry DH, Wells C, Collins-Burow B, Burow ME. Novel application of the published kinase inhibitor set to identify therapeutic targets and pathways in triple negative breast cancer subtypes. PLoS One. 2017 Aug 3;12(8):e0177802. doi: 10.1371/journal.pone.0177802. eCollection 2017. PMID: 28771473

Drewry DH, Wells CI, Andrews DM, Angell R, Al-Ali H, Axtman AD, Capuzzi SJ, Elkins JM, Ettmayer P, Frederiksen M, Gileadi O, Gray N, Hooper A, Knapp S, Laufer S, Luecking U, Michaelides M, Müller S, Muratov E, Denny RA, Saikatendu KS, Treiber DK, Zuercher WJ, Willson TM. Progress towards a public chemogenomic set for protein kinases and a call for contributions. PLoS One. 2017 Aug 2;12(8):e0181585. doi: 10.1371/journal.pone.0181585. eCollection 2017.
PMID: 28767711

2016

Cestari I, Haas P, Moretti NS, Schenkman S, Stuart K. Chemogenetic Characterization of Inositol Phosphate Metabolic Pathway Reveals Druggable Enzymes for Targeting Kinetoplastid Parasites. Cell Chem Biol. 2016
May 19;23(5):608-617. doi: 10.1016/j.chembiol.2016.03.015. Epub 2016 Apr 28. PMID: 27133314

Rodriguez DA, Weinlich R, Brown S, Guy C, Fitzgerald P, Dillon CP, Oberst A, Quarato G, Low J, Cripps JG, Chen T, Green DR. Characterization of RIPK3-mediated phosphorylation of the activation loop of MLKL during necroptosis. Cell Death Differ. 2016 Jan;23(1):76-88. doi: 10.1038/cdd.2015.70. Epub 2015 May 29. PMID: 26024392

Elkins JM, Fedele V, Szklarz M, Abdul Azeez KR, Salah E, Mikolajczyk J, Romanov S, Sepetov N, Huang XP, Roth BL, Al Haj Zen A, Fourches D, Muratov E, Tropsha A, Morris J, Teicher BA, Kunkel M, Polley E, Lackey KE, Atkinson FL, Overington JP, Bamborough P, Müller S, Price DJ, Willson TM, Drewry DH, Knapp S, Zuercher WJ. Comprehensive characterization of the Published Kinase Inhibitor Set. Nat Biotechnol. 2016 Jan;34(1):95-103. doi: 10.1038/nbt.3374. Epub 2015 Oct 26. PMID: 26501955

Long T, Neitz RJ, Beasley R, Kalyanaraman C, Suzuki BM, Jacobson MP, Dissous C, McKerrow JH, Drewry DH, Zuercher WJ, Singh R, Caffrey CR. Structure-Bioactivity Relationship for Benzimidazole Thiophene Inhibitors of Polo-Like Kinase 1 (PLK1), a Potential Drug Target in Schistosoma mansoni. PLoS Negl Trop Dis. 2016 Jan 11;10(1):e0004356. doi: 10.1371/journal.pntd.0004356. eCollection 2016 Jan. PMID: 26751972

Simpson C, Jones NG, Hull-Ryde EA, Kireev D, Stashko M, Tang K, Janetka J, Wildman SA, Zuercher WJ, Schapira M, Hui R, Janzen W, Sibley LD. Identification of small molecule inhibitors that block the Toxoplasma gondii rhoptry kinase ROP18. ACS Infect Dis. 2016 Mar 11;2(3):194-206. Epub 2015 Dec 28. PMID: 27379343

Amata E, Xi H, Colmenarejo G, Gonzalez-Diaz R, Cordon-Obras C, Berlanga M, Manzano P, Erath J, Roncal NE, Lee PJ, Leed SE, Rodriguez A, Sciotti RJ, Navarro M, Pollastri MP. Identification of "Preferred" Human Kinase Inhibitors for Sleeping Sickness Lead Discovery. Are Some Kinases Better than Others for Inhibitor Repurposing? ACS Infect Dis. 2016 Mar 11;2(3):180-186. Epub 2016 Jan 17. PMID: 26998514

Scheipl S, Barnard M, Cottone L, Jorgensen M, Drewry DH, Zuercher WJ, Turlais F, Ye H, Leite AP, Smith JA, Leithner A, Möller P, Brüderlein S, Guppy N, Amary F, Tirabosco R, Strauss SJ, Pillay N, Flanagan AM. EGFR inhibitors identified as a potential treatment for chordoma in a focused compound screen. J Pathol. 2016 Jul;239(3):320-34.
doi: 10.1002/path.4729. Epub 2016 May 31. PMID: 27102572

Sidik SM, Hortua Triana MA, Paul AS, El Bakkouri M, Hackett CG, Tran F, Westwood NJ, Hui R, Zuercher WJ, Duraisingh MT, Moreno SN, Lourido S. Using a Genetically Encoded Sensor to Identify Inhibitors of Toxoplasma gondii Ca2+ Signaling. J Biol Chem. 2016 Apr 29;291(18):9566-80. doi:10.1074/jbc.M115.703546. Epub 2016 Mar 1. PMID: 26933036

2015

Homan KT, Larimore KM, Elkins JM, Szklarz M, Knapp S, Tesmer JJ. Identification and structure-function analysis of subfamily selective G protein-coupled receptor kinase inhibitors. ACS Chem Biol. 2015 Jan 16;10(1):310-9. doi: 10.1021/cb5006323. Epub 2014 Oct 3. PMID: 25238254

Thorne CA, Wichaidit C, Coster AD, Posner BA, Wu LF, Altschuler SJ. GSK-3 modulates cellular responses to a broad spectrum of kinase inhibitors. Nat Chem Biol. 2015 Jan;11(1):58-63. doi: 10.1038/nchembio.1690. Epub 2014 Nov 17. PMID: 25402767

Richters A, Basu D, Engel J, Ercanoglu MS, Balke-Want H, Tesch R, Thomas RK, Rauh D. Identification and further development of potent TBK1 inhibitors. ACS Chem Biol. 2015 Jan 16;10(1):289-98. doi: 10.1021/cb500908d.
PMID: 25540906

Lipchik AM, Perez M, Bolton S, Dumrongprechachan V, Ouellette SB, Cui W, Parker LL. KINATEST-ID: a pipeline to develop phosphorylation-dependent terbium sensitizing kinase assays. J Am Chem Soc. 2015
Feb 25;137(7):2484-94. doi: 10.1021/ja507164a. Epub 2015 Feb 17. PMID: 25689372

Al-Ali H, Lee DH, Danzi MC, Nassif H, Gautam P, Wennerberg K, Zuercher B, Drewry DH, Lee JK, Lemmon VP, Bixby JL. Rational Polypharmacology: Systematically Identifying and Engaging Multiple Drug Targets To Promote Axon Growth.ACS Chem Biol. 2015 Aug 21;10(8):1939-51. doi: 10.1021/acschembio.5b00289. Epub 2015 Jun 24. PMID: 26056718

Urick AK, Hawk LM, Cassel MK, Mishra NK, Liu S, Adhikari N, Zhang W, dos Santos CO, Hall JL, Pomerantz WC. Dual Screening of BPTF and Brd4 Using Protein-Observed Fluorine NMR Uncovers New Bromodomain Probe Molecules. ACS Chem Biol. 2015 Oct 16;10(10):2246-56. doi: 10.1021/acschembio.5b00483. Epub 2015 Jul 28. PMID: 26158404

Szwajda A, Gautam P, Karhinen L, Jha SK, Saarela J, Shakyawar S, Turunen L, Yadav B, Tang J, Wennerberg K, Aittokallio T. Systematic Mapping of Kinase Addiction Combinations in Breast Cancer Cells by Integrating Drug Sensitivity and Selectivity Profiles. Chem Biol. 2015 Aug 20;22(8):1144-55. doi: 10.1016/j.chembiol.2015.06.021. Epub 2015 Jul 23. PMID: 26211361

Mardilovich K, Baugh M, Crighton D, Kowalczyk D, Gabrielsen M, Munro J, Croft DR, Lourenco F, James D, Kalna G, McGarry L, Rath O, Shanks E, Garnett MJ, McDermott U, Brookfield J, Charles M, Hammonds T, Olson MF. LIM kinase inhibitors disrupt mitotic microtubule organization and impair tumor cell proliferation. Oncotarget. 2015 Nov 17;6(36):38469-86. doi: 10.18632/oncotarget.6288. PMID: 26540348

Guidi A, Mansour NR, Paveley RA, Carruthers IM, Besnard J, Hopkins AL, Gilbert IH, Bickle QD. Application of RNAi to Genomic Drug Target Validation in Schistosomes. PLoS Negl Trop Dis. 2015 May 20;9(5):e0003801. doi: 10.1371/journal.pntd.0003801. eCollection 2015 May. PMID: 25992548

2014

Derbyshire ER, Zuzarte-Luís V, Magalhães AD, Kato N, Sanschagrin PC, Wang J, Zhou W, Miduturu CV, Mazitschek R, Sliz P, Mota MM, Gray NS, Clardy J. Chemical interrogation of the malaria kinome. Chembiochem. 2014 Sep 5;15(13):1920-30. doi: 10.1002/cbic.201400025. Epub 2014 Aug 8. PMID: 25111632

Hildebrand JM, Tanzer MC, Lucet IS, Young SN, Spall SK, Sharma P, Pierotti C, Garnier JM, Dobson RC, Webb AI, Tripaydonis A, Babon JJ, Mulcair MD, Scanlon MJ, Alexander WS, Wilks AF, Czabotar PE, Lessene G, Murphy JM, Silke J. Activation of the pseudokinase MLKL unleashes the four-helix bundle domain to induce membrane localization and necroptotic cell death. Proc Natl Acad Sci U S A. 2014 Oct 21;111(42):15072-7. doi: 10.1073/pnas.1408987111. Epub 2014 Oct 6. PMID: 25288762

Ember SW, Zhu JY, Olesen SH, Martin MP, Becker A, Berndt N, Georg GI, Schönbrunn E. Acetyl-lysine binding site of bromodomain-containing protein 4 (BRD4) interacts with diverse kinase inhibitors. ACS Chem Biol. 2014 May 16;9(5):1160-71. doi: 10.1021/cb500072z. Epub 2014 Mar 13. PMID: 24568369

Diaz R, Luengo-Arratta SA, Seixas JD, Amata E, Devine W, Cordon-Obras C, Rojas-Barros DI, Jimenez E, Ortega F, Crouch S, Colmenarejo G, Fiandor JM, Martin JJ, Berlanga M, Gonzalez S, Manzano P, Navarro M, Pollastri MP. Identification and characterization of hundreds of potent and selective inhibitors of Trypanosoma brucei growth from a kinase-targeted library screening campaign. PLoS Negl Trop Dis. 2014 Oct 23;8(10):e3253. doi: 10.1371/journal.pntd.0003253. eCollection 2014 Oct. PMID: 25340575

Ramamoorthi R, Graef KM, Krattiger A, Dent JC. WIPO re:search: catalyzing collaborations to accelerate product development for diseases of poverty. Chem Rev. 2014 Nov 26;114(22):11272-9. doi: 10.1021/cr5000656. Epub 2014 Sep 17. Review. No abstract available. PMID: 25229276

Guo K, Shelat AA, Guy RK, Kastan MB. Development of a cell-based, high-throughput screening assay for ATM kinase inhibitors. J Biomol Screen. 2014 Apr;19(4):538-46. doi: 10.1177/1087057113520325. Epub 2014 Jan 24. Erratum in: J Biomol Screen. 2014 Dec;19(10):1418. PMID: 24464432

2013

Dranchak P, MacArthur R, Guha R, Zuercher WJ, Drewry DH, Auld DS, Inglese J. Profile of the GSK published protein kinase inhibitor set across ATP-dependent and-independent luciferases: implications for reporter-gene assays. PLoS One. 2013;8(3):e57888. doi: 10.1371/journal.pone.0057888. Epub 2013 Mar 7. PMID: 2350544

Knapp S, Arruda P, Blagg J, Burley S, Drewry DH, Edwards A, Fabbro D, Gillespie P, Gray NS, Kuster B, Lackey KE, Mazzafera P, Tomkinson NC, Willson TM, Workman P, Zuercher WJ. A public-private partnership to unlock the untargeted kinome. Nat Chem Biol. 2013 Jan;9(1):3-6. doi: 10.1038/nchembio.1113. No abstract available. PMID: 23238671

Patel PR, Sun H, Li SQ, Shen M, Khan J, Thomas CJ, Davis MI. Identification of potent Yes1 kinase inhibitors using a library screening approach. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4398-403. doi: 10.1016/j.bmcl.2013.05.072. Epub 2013 May 29. PMID: 23787099

Drewry DH, Willson TM, Zuercher WJ. Seeding collaborations to advance kinase science with the GSK Published Kinase Inhibitor Set (PKIS). Curr Top Med Chem. 2014;14(3):340-2. Review. PMID: 24283969

2011

Atkinson JM, Shelat AA, Carcaboso AM, Kranenburg TA, Arnold LA, Boulos N, Wright K, Johnson RA, Poppleton H, Mohankumar KM, Féau C, Phoenix T, Gibson P, Zhu L, Tong Y, Eden C, Ellison DW, Priebe W, Koul D, Yung WK, Gajjar A, Stewart CF, Guy RK, Gilbertson RJ. An integrated in vitro and in vivo high-throughput screen identifies treatment leads for ependymoma. Cancer Cell. 2011 Sep 13;20(3):384-99. doi: 10.1016/j.ccr.2011.08.013. PMID: 21907928