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Page 1
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. Among authors: planken s. 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.
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: planken 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 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. 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 Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19.
Hoffman RL, Kania RS, Brothers MA, Davies JF, Ferre RA, Gajiwala KS, He M, Hogan RJ, Kozminski K, Li LY, Lockner JW, Lou J, Marra MT, Mitchell LJ Jr, Murray BW, Nieman JA, Noell S, Planken SP, Rowe T, Ryan K, Smith GJ 3rd, Solowiej JE, Steppan CM, Taggart B. Hoffman RL, et al. Among authors: planken sp. J Med Chem. 2020 Nov 12;63(21):12725-12747. doi: 10.1021/acs.jmedchem.0c01063. Epub 2020 Oct 15. J Med Chem. 2020. PMID: 33054210
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: planken s. 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
Effective targeting of Hedgehog signaling in a medulloblastoma model with PF-5274857, a potent and selective Smoothened antagonist that penetrates the blood-brain barrier.
Rohner A, Spilker ME, Lam JL, Pascual B, Bartkowski D, Li QJ, Yang AH, Stevens G, Xu M, Wells PA, Planken S, Nair S, Sun S. Rohner A, et al. Among authors: planken s. Mol Cancer Ther. 2012 Jan;11(1):57-65. doi: 10.1158/1535-7163.MCT-11-0691. Epub 2011 Nov 14. Mol Cancer Ther. 2012. PMID: 22084163
Efficacy and Imaging-Enabled Pharmacodynamic Profiling of KRAS G12C Inhibitors in Xenograft and Genetically Engineered Mouse Models of Cancer.
Lee C, Jiang ZK, Planken S, Manzuk LK, Ortiz R, Hall M, Noorbehesht K, Ram S, Affolter T, Troche GE, Ihle NT, Johnson T, Ahn Y, Kraus M, Giddabasappa A. Lee C, et al. Among authors: planken s. Mol Cancer Ther. 2023 Jul 5;22(7):891-900. doi: 10.1158/1535-7163.MCT-22-0810. Mol Cancer Ther. 2023. PMID: 37186518 Free PMC article.
Novel selective inhibitors of neutral endopeptidase for the treatment of female sexual arousal disorder. Synthesis and activity of functionalized glutaramides.
Pryde DC, Maw GN, Planken S, Platts MY, Sanderson V, Corless M, Stobie A, Barber CG, Russell R, Foster L, Barker L, Wayman C, Van Der Graaf P, Stacey P, Morren D, Kohl C, Beaumont K, Coggon S, Tute M. Pryde DC, et al. Among authors: planken s. J Med Chem. 2006 Jul 13;49(14):4409-24. doi: 10.1021/jm060133g. J Med Chem. 2006. PMID: 16821800
15 results