KCGS, PKIS2, and PKIS Publications

2018

Covalent inhibitors of EGFR family protein kinases induce degradation of human Tribbles 2 (TRIB2) pseudokinase in cancer cells. Foulkes DM, Byrne DP, Yeung W, Shrestha S, Bailey FP, Ferries S, Eyers CE, Keeshan K, Wells C, Drewry DH, Zuercher WJ, Kannan N, Eyers PA. Sci Signal. 2018 Sep 25;11(549). pii: eaat7951. doi: 10.1126/scisignal.aat7951. PMID: 30254057

New tools for carbohydrate sulphation analysis: Heparan Sulphate 2- O -sulphotransferase (HS2ST) is a target for small molecule protein kinase inhibitors. 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. Biochem J. 2018 Jun 22. pii: BCJ20180265. doi: 10.1042/BCJ20180265. [Epub ahead of print] PMID: 29934491

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

Identification of PKMYT1 inhibitors by screening the GSK published protein kinase inhibitor set I and II. Platzer C, Najjar A, Rhoe A, Erdmann F, Sippl W, Schmidt M. 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

Immuno-detection by sequencing enables large-scale high-dimensional phenotyping in cells. 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. Nat Commun. 2018 Jun 19;9(1):2384. doi: 10.1038/s41467-018-04761-0. PMID: 29921844

Application of Integrated Drug Screening/Kinome Analysis to Identify Inhibitors of Gemcitabine-Resistant Pancreatic Cancer Cell Growth. 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. SLAS Discov. 2018 May 1:2472555218773045. doi: 10.1177/2472555218773045. [Epub ahead of print] PMID: 29742358

The polo-like kinase 1 inhibitor volasertib synergistically increases radiation efficacy in glioma stem cells. Dong J, Park SY, Nguyen N, Ezhilarasan R, Martinez-Ledesma E, Wu S, Henry V, Piao Y, Tiao N, Brunell D, Stephan C, Verhaak R, Sulman E, Balasubramaniyan V, de Groot JF. Oncotarget. 2018 Jan 8;9(12):10497-10509. doi: 10.18632/oncotarget.24041. eCollection 2018 Feb 13. PMID: 29535822

2017

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

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

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

Tension Creates an Endoreplication Wavefront that Leads Regeneration of Epicardial Tissue. 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. Dev Cell. 2017 Sep 25;42(6):600-615.e4. doi: 10.1016/j.devcel.2017.08.024. PMID: 28950101

Systematic Kinase Inhibitor Profiling Identifies CDK9 as a Synthetic Lethal Target in NUT Midline Carcinoma. 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. Cell Rep. 2017 Sep 19;20(12):2833-2845. doi: 10.1016/j.celrep.2017.08.082. PMID: 28930680

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

Functional annotation of chemical libraries across diverse biological processes. 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. 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

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

Progress towards a public chemogenomic set for protein kinases and a call for contributions. 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. PLoS One. 2017 Aug 2;12(8):e0181585. doi: 10.1371/journal.pone.0181585. eCollection 2017. PMID: 28767711

Prediction of intracellular exposure bridges the gap between target- and cell-based drug discovery. 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. 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

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

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. Khan AS, Murray MJ, Ho CMK, Zuercher WJ, Reeves MB, Strang BL. J Gen Virol. 2017 Apr;98(4):754-768. doi: 10.1099/jgv.0.000713. Epub 2017 Apr 20. PMID: 28100301

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

2016

EGFR inhibitors identified as a potential treatment for chordoma in a focused compound screen. 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. J Pathol. 2016 Jul;239(3):320-34. doi: 10.1002/path.4729. Epub 2016 May 31. PMID: 27102572

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

Using a Genetically Encoded Sensor to Identify Inhibitors of Toxoplasma gondii Ca2+ Signaling. 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. J Biol Chem. 2016 Apr 29;291(18):9566-80. doi:10.1074/jbc.M115.703546. Epub 2016 Mar 1. PMID: 26933036

Identification of "Preferred" Human Kinase Inhibitors for Sleeping Sickness Lead Discovery. Are Some Kinases Better than Others for Inhibitor Repurposing? 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. ACS Infect Dis. 2016 Mar 11;2(3):180-186. Epub 2016 Jan 17. PMID: 26998514

Identification of small molecule inhibitors that block the Toxoplasma gondii rhoptry kinase ROP18. 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. ACS Infect Dis. 2016 Mar 11;2(3):194-206. Epub 2015 Dec 28. PMID: 27379343

Comprehensive characterization of the Published Kinase Inhibitor Set. 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. Nat Biotechnol. 2016 Jan;34(1):95-103. doi: 10.1038/nbt.3374. Epub 2015 Oct 26. PMID: 26501955

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

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

2015

LIM kinase inhibitors disrupt mitotic microtubule organization and impair tumor cell proliferation. 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. Oncotarget. 2015 Nov 17;6(36):38469-86. doi: 10.18632/oncotarget.6288. PMID: 26540348

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

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

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

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

Low cost whole-organism screening of compounds for anthelmintic activity. Preston S, Jabbar A, Nowell C, Joachim A, Ruttkowski B, Baell J, Cardno T, Korhonen PK, Piedrafita D, Ansell BR, Jex AR, Hofmann A, Gasser RB. Int J Parasitol. 2015 Apr;45(5):333-43. doi: 10.1016/j.ijpara.2015.01.007. Epub 2015 Mar 5. PMID: 25746136

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

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

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

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

2014

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

Cellular manganese content is developmentally regulated in human dopaminergic neurons. Kumar KK, Lowe EW Jr, Aboud AA, Neely MD, Redha R, Bauer JA, Odak M, Weaver CD, Meiler J, Aschner M, Bowman AB. Sci Rep. 2014 Oct 28;4:6801. doi: 10.1038/srep06801. PMID: 25348053

Identification and characterization of hundreds of potent and selective inhibitors of Trypanosoma brucei growth from a kinase-targeted library screening campaign. 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. PLoS Negl Trop Dis. 2014 Oct 23;8(10):e3253. doi: 10.1371/journal.pntd.0003253. eCollection 2014 Oct. PMID: 25340575

Activation of the pseudokinase MLKL unleashes the four-helix bundle domain to induce membrane localization and necroptotic cell death. 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. 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

Chemical interrogation of the malaria kinome. 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. Chembiochem. 2014 Sep 5;15(13):1920-30. doi: 10.1002/cbic.201400025. Epub 2014 Aug 8. PMID: 25111632

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

Development of a cell-based, high-throughput screening assay for ATM kinase inhibitors. Guo K, Shelat AA, Guy RK, Kastan MB. 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

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

2013

Identification of potent Yes1 kinase inhibitors using a library screening approach. Patel PR, Sun H, Li SQ, Shen M, Khan J, Thomas CJ, Davis MI. 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

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

A public-private partnership to unlock the untargeted kinome. 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. Nat Chem Biol. 2013 Jan;9(1):3-6. doi: 10.1038/nchembio.1113. No abstract available. PMID: 23238671

2011

An integrated in vitro and in vivo high-throughput screen identifies treatment leads for ependymoma. 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. Cancer Cell. 2011 Sep 13;20(3):384-99. doi: 10.1016/j.ccr.2011.08.013. PMID: 21907928