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Expanding control of the tumor cell cycle with a CDK2/4/6 inhibitor.
Freeman-Cook K, Hoffman RL, Miller N, Almaden J, Chionis J, Zhang Q, Eisele K, Liu C, Zhang C, Huser N, Nguyen L, Costa-Jones C, Niessen S, Carelli J, Lapek J, Weinrich SL, Wei P, McMillan E, Wilson E, Wang TS, McTigue M, Ferre RA, He YA, Ninkovic S, Behenna D, Tran KT, Sutton S, Nagata A, Ornelas MA, Kephart SE, Zehnder LR, Murray B, Xu M, Solowiej JE, Visswanathan R, Boras B, Looper D, Lee N, Bienkowska JR, Zhu Z, Kan Z, Ding Y, Mu XJ, Oderup C, Salek-Ardakani S, White MA, VanArsdale T, Dann SG. Freeman-Cook K, et al. Among authors: kephart se. Cancer Cell. 2021 Oct 11;39(10):1404-1421.e11. doi: 10.1016/j.ccell.2021.08.009. Epub 2021 Sep 13. Cancer Cell. 2021. PMID: 34520734 Free article.
Discovery of PF-06873600, a CDK2/4/6 Inhibitor for the Treatment of Cancer.
Freeman-Cook KD, Hoffman RL, Behenna DC, Boras B, Carelli J, Diehl W, Ferre RA, He YA, Hui A, Huang B, Huser N, Jones R, Kephart SE, Lapek J, McTigue M, Miller N, Murray BW, Nagata A, Nguyen L, Niessen S, Ninkovic S, O'Doherty I, Ornelas MA, Solowiej J, Sutton SC, Tran K, Tseng E, Visswanathan R, Xu M, Zehnder L, Zhang Q, Zhang C, Dann S. Freeman-Cook KD, et al. Among authors: kephart se. J Med Chem. 2021 Jul 8;64(13):9056-9077. doi: 10.1021/acs.jmedchem.1c00159. Epub 2021 Jun 10. J Med Chem. 2021. PMID: 34110834
Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195).
Cheng H, Orr STM, Bailey S, Brooun A, Chen P, Deal JG, Deng YL, Edwards MP, Gallego GM, Grodsky N, Huang B, Jalaie M, Kaiser S, Kania RS, Kephart SE, Lafontaine J, Ornelas MA, Pairish M, Planken S, Shen H, Sutton S, Zehnder L, Almaden CD, Bagrodia S, Falk MD, Gukasyan HJ, Ho C, Kang X, Kosa RE, Liu L, Spilker ME, Timofeevski S, Visswanathan R, Wang Z, Meng F, Ren S, Shao L, Xu F, Kath JC. Cheng H, et al. Among authors: kephart se. J Med Chem. 2021 Jan 14;64(1):644-661. doi: 10.1021/acs.jmedchem.0c01652. Epub 2020 Dec 24. J Med Chem. 2021. PMID: 33356246
SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance.
Jensen-Pergakes K, Tatlock J, Maegley KA, McAlpine IJ, McTigue M, Xie T, Dillon CP, Wang Y, Yamazaki S, Spiegel N, Shi M, Nemeth A, Miller N, Hendrickson E, Lam H, Sherrill J, Chung CY, McMillan EA, Bryant SK, Palde P, Braganza J, Brooun A, Deng YL, Goshtasbi V, Kephart SE, Kumpf RA, Liu W, Patman RL, Rui E, Scales S, Tran-Dube M, Wang F, Wythes M, Paul TA. Jensen-Pergakes K, et al. Among authors: kephart se. Mol Cancer Ther. 2022 Jan;21(1):3-15. doi: 10.1158/1535-7163.MCT-21-0620. Epub 2021 Nov 4. Mol Cancer Ther. 2022. PMID: 34737197
Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497).
Kung PP, Bingham P, Brooun A, Collins M, Deng YL, Dinh D, Fan C, Gajiwala KS, Grantner R, Gukasyan HJ, Hu W, Huang B, Kania R, Kephart SE, Krivacic C, Kumpf RA, Khamphavong P, Kraus M, Liu W, Maegley KA, Nguyen L, Ren S, Richter D, Rollins RA, Sach N, Sharma S, Sherrill J, Spangler J, Stewart AE, Sutton S, Uryu S, Verhelle D, Wang H, Wang S, Wythes M, Xin S, Yamazaki S, Zhu H, Zhu J, Zehnder L, Edwards M. Kung PP, et al. Among authors: kephart se. J Med Chem. 2018 Feb 8;61(3):650-665. doi: 10.1021/acs.jmedchem.7b01375. Epub 2017 Dec 27. J Med Chem. 2018. PMID: 29211475
Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth.
Murray BW, Guo C, Piraino J, Westwick JK, Zhang C, Lamerdin J, Dagostino E, Knighton D, Loi CM, Zager M, Kraynov E, Popoff I, Christensen JG, Martinez R, Kephart SE, Marakovits J, Karlicek S, Bergqvist S, Smeal T. Murray BW, et al. Among authors: kephart se. Proc Natl Acad Sci U S A. 2010 May 18;107(20):9446-51. doi: 10.1073/pnas.0911863107. Epub 2010 May 3. Proc Natl Acad Sci U S A. 2010. PMID: 20439741 Free PMC article.