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A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo.
Olivero AG, Eigenbrot C, Goldsmith R, Robarge K, Artis DR, Flygare J, Rawson T, Sutherlin DP, Kadkhodayan S, Beresini M, Elliott LO, DeGuzman GG, Banner DW, Ultsch M, Marzec U, Hanson SR, Refino C, Bunting S, Kirchhofer D. Olivero AG, et al. J Biol Chem. 2005 Mar 11;280(10):9160-9. doi: 10.1074/jbc.M409068200. Epub 2005 Jan 4. J Biol Chem. 2005. PMID: 15632123 Free article.
Small-molecule pan-IAP antagonists: a patent review.
Flygare JA, Fairbrother WJ. Flygare JA, et al. Expert Opin Ther Pat. 2010 Feb;20(2):251-67. doi: 10.1517/13543770903567077. Expert Opin Ther Pat. 2010. PMID: 20100005 Review.
Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres.
Cohen F, Koehler MF, Bergeron P, Elliott LO, Flygare JA, Franklin MC, Gazzard L, Keteltas SF, Lau K, Ly CQ, Tsui V, Fairbrother WJ. Cohen F, et al. Among authors: flygare ja. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2229-33. doi: 10.1016/j.bmcl.2010.02.021. Epub 2010 Feb 8. Bioorg Med Chem Lett. 2010. PMID: 20189383
Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
Flygare JA, Beresini M, Budha N, Chan H, Chan IT, Cheeti S, Cohen F, Deshayes K, Doerner K, Eckhardt SG, Elliott LO, Feng B, Franklin MC, Reisner SF, Gazzard L, Halladay J, Hymowitz SG, La H, LoRusso P, Maurer B, Murray L, Plise E, Quan C, Stephan JP, Young SG, Tom J, Tsui V, Um J, Varfolomeev E, Vucic D, Wagner AJ, Wallweber HJ, Wang L, Ware J, Wen Z, Wong H, Wong JM, Wong M, Wong S, Yu R, Zobel K, Fairbrother WJ. Flygare JA, et al. J Med Chem. 2012 May 10;55(9):4101-13. doi: 10.1021/jm300060k. Epub 2012 Mar 28. J Med Chem. 2012. PMID: 22413863 Free PMC article.
43 results