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Page 1
Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR.
Planken S, Behenna DC, Nair SK, Johnson TO, Nagata A, Almaden C, Bailey S, Ballard TE, Bernier L, Cheng H, Cho-Schultz S, Dalvie D, Deal JG, Dinh DM, Edwards MP, Ferre RA, Gajiwala KS, Hemkens M, Kania RS, Kath JC, Matthews J, Murray BW, Niessen S, Orr ST, Pairish M, Sach NW, Shen H, Shi M, Solowiej J, Tran K, Tseng E, Vicini P, Wang Y, Weinrich SL, Zhou R, Zientek M, Liu L, Luo Y, Xin S, Zhang C, Lafontaine J. Planken S, et al. Among authors: niessen s. J Med Chem. 2017 Apr 13;60(7):3002-3019. doi: 10.1021/acs.jmedchem.6b01894. Epub 2017 Mar 29. J Med Chem. 2017. PMID: 28287730
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.
Cheng H, Nair SK, Murray BW, Almaden C, Bailey S, Baxi S, Behenna D, Cho-Schultz S, Dalvie D, Dinh DM, Edwards MP, Feng JL, Ferre RA, Gajiwala KS, Hemkens MD, Jackson-Fisher A, Jalaie M, Johnson TO, Kania RS, Kephart S, Lafontaine J, Lunney B, Liu KK, Liu Z, Matthews J, Nagata A, Niessen S, Ornelas MA, Orr ST, Pairish M, Planken S, Ren S, Richter D, Ryan K, Sach N, Shen H, Smeal T, Solowiej J, Sutton S, Tran K, Tseng E, Vernier W, Walls M, Wang S, Weinrich SL, Xin S, Xu H, Yin MJ, Zientek M, Zhou R, Kath JC. Cheng H, et al. Among authors: niessen s. J Med Chem. 2016 Mar 10;59(5):2005-24. doi: 10.1021/acs.jmedchem.5b01633. Epub 2016 Jan 28. J Med Chem. 2016. PMID: 26756222
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: niessen s. 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
Proteome-wide Map of Targets of T790M-EGFR-Directed Covalent Inhibitors.
Niessen S, Dix MM, Barbas S, Potter ZE, Lu S, Brodsky O, Planken S, Behenna D, Almaden C, Gajiwala KS, Ryan K, Ferre R, Lazear MR, Hayward MM, Kath JC, Cravatt BF. Niessen S, et al. Cell Chem Biol. 2017 Nov 16;24(11):1388-1400.e7. doi: 10.1016/j.chembiol.2017.08.017. Epub 2017 Sep 28. Cell Chem Biol. 2017. PMID: 28965727 Free PMC article.
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: niessen s. 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.
[No title available]
[No authors listed] [No authors listed] PMID: 33428942
A road map to evaluate the proteome-wide selectivity of covalent kinase inhibitors.
Lanning BR, Whitby LR, Dix MM, Douhan J, Gilbert AM, Hett EC, Johnson TO, Joslyn C, Kath JC, Niessen S, Roberts LR, Schnute ME, Wang C, Hulce JJ, Wei B, Whiteley LO, Hayward MM, Cravatt BF. Lanning BR, et al. Among authors: niessen s. Nat Chem Biol. 2014 Sep;10(9):760-767. doi: 10.1038/nchembio.1582. Epub 2014 Jul 13. Nat Chem Biol. 2014. PMID: 25038787 Free PMC article.
Chemoselective Preparation of Clickable Aryl Sulfonyl Fluoride Monomers: A Toolbox of Highly Functionalized Intermediates for Chemical Biology Probe Synthesis.
Fadeyi O, Parikh MD, Chen MZ, Kyne RE Jr, Taylor AP, O'Doherty I, Kaiser SE, Barbas S, Niessen S, Shi M, Weinrich SL, Kath JC, Jones LH, Robinson RP. Fadeyi O, et al. Among authors: niessen s. Chembiochem. 2016 Oct 17;17(20):1925-1930. doi: 10.1002/cbic.201600427. Epub 2016 Aug 30. Chembiochem. 2016. PMID: 27504718
151 results