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Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.
Lee KL, Ambler CM, Anderson DR, Boscoe BP, Bree AG, Brodfuehrer JI, Chang JS, Choi C, Chung S, Curran KJ, Day JE, Dehnhardt CM, Dower K, Drozda SE, Frisbie RK, Gavrin LK, Goldberg JA, Han S, Hegen M, Hepworth D, Hope HR, Kamtekar S, Kilty IC, Lee A, Lin LL, Lovering FE, Lowe MD, Mathias JP, Morgan HM, Murphy EA, Papaioannou N, Patny A, Pierce BS, Rao VR, Saiah E, Samardjiev IJ, Samas BM, Shen MWH, Shin JH, Soutter HH, Strohbach JW, Symanowicz PT, Thomason JR, Trzupek JD, Vargas R, Vincent F, Yan J, Zapf CW, Wright SW. Lee KL, et al. Among authors: kamtekar s. J Med Chem. 2017 Jul 13;60(13):5521-5542. doi: 10.1021/acs.jmedchem.7b00231. Epub 2017 Jun 14. J Med Chem. 2017. PMID: 28498658
Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode.
Meyers MJ, Pelc M, Kamtekar S, Day J, Poda GI, Hall MK, Michener ML, Reitz BA, Mathis KJ, Pierce BS, Parikh MD, Mischke DA, Long SA, Parlow JJ, Anderson DR, Thorarensen A. Meyers MJ, et al. Among authors: kamtekar s. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1543-7. doi: 10.1016/j.bmcl.2010.01.078. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20137931
Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 2. Discovery of 7-azaspiro[3.5]nonane urea PF-04862853, an orally efficacious inhibitor of fatty acid amide hydrolase (FAAH) for pain.
Meyers MJ, Long SA, Pelc MJ, Wang JL, Bowen SJ, Schweitzer BA, Wilcox MV, McDonald J, Smith SE, Foltin S, Rumsey J, Yang YS, Walker MC, Kamtekar S, Beidler D, Thorarensen A. Meyers MJ, et al. Among authors: kamtekar s. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6545-53. doi: 10.1016/j.bmcl.2011.08.048. Epub 2011 Aug 19. Bioorg Med Chem Lett. 2011. PMID: 21924613
Crystallization and preliminary X-ray diffraction analysis of rat autotaxin.
Day JE, Hall T, Pegg LE, Benson TE, Hausmann J, Kamtekar S. Day JE, et al. Among authors: kamtekar s. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2010 Sep 1;66(Pt 9):1127-9. doi: 10.1107/S1744309110030228. Epub 2010 Aug 31. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2010. PMID: 20823544 Free PMC article.
Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain.
Ahn K, Johnson DS, Mileni M, Beidler D, Long JZ, McKinney MK, Weerapana E, Sadagopan N, Liimatta M, Smith SE, Lazerwith S, Stiff C, Kamtekar S, Bhattacharya K, Zhang Y, Swaney S, Van Becelaere K, Stevens RC, Cravatt BF. Ahn K, et al. Among authors: kamtekar s. Chem Biol. 2009 Apr 24;16(4):411-20. doi: 10.1016/j.chembiol.2009.02.013. Chem Biol. 2009. PMID: 19389627 Free PMC article.
Structural basis of substrate discrimination and integrin binding by autotaxin.
Hausmann J, Kamtekar S, Christodoulou E, Day JE, Wu T, Fulkerson Z, Albers HM, van Meeteren LA, Houben AJ, van Zeijl L, Jansen S, Andries M, Hall T, Pegg LE, Benson TE, Kasiem M, Harlos K, Kooi CW, Smyth SS, Ovaa H, Bollen M, Morris AJ, Moolenaar WH, Perrakis A. Hausmann J, et al. Among authors: kamtekar s. Nat Struct Mol Biol. 2011 Feb;18(2):198-204. doi: 10.1038/nsmb.1980. Epub 2011 Jan 16. Nat Struct Mol Biol. 2011. PMID: 21240271 Free PMC article.
Structure-guided inhibitor design for human FAAH by interspecies active site conversion.
Mileni M, Johnson DS, Wang Z, Everdeen DS, Liimatta M, Pabst B, Bhattacharya K, Nugent RA, Kamtekar S, Cravatt BF, Ahn K, Stevens RC. Mileni M, et al. Among authors: kamtekar s. Proc Natl Acad Sci U S A. 2008 Sep 2;105(35):12820-4. doi: 10.1073/pnas.0806121105. Epub 2008 Aug 27. Proc Natl Acad Sci U S A. 2008. PMID: 18753625 Free PMC article.
Kinetic and structural characterization of caspase-3 and caspase-8 inhibition by a novel class of irreversible inhibitors.
Wang Z, Watt W, Brooks NA, Harris MS, Urban J, Boatman D, McMillan M, Kahn M, Heinrikson RL, Finzel BC, Wittwer AJ, Blinn J, Kamtekar S, Tomasselli AG. Wang Z, et al. Among authors: kamtekar s. Biochim Biophys Acta. 2010 Sep;1804(9):1817-31. doi: 10.1016/j.bbapap.2010.05.007. Epub 2010 May 24. Biochim Biophys Acta. 2010. PMID: 20580860
31 results