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Identification of novel HSP90α/β isoform selective inhibitors using structure-based drug design. demonstration of potential utility in treating CNS disorders such as Huntington's disease.
Ernst JT, Neubert T, Liu M, Sperry S, Zuccola H, Turnbull A, Fleck B, Kargo W, Woody L, Chiang P, Tran D, Chen W, Snyder P, Alcacio T, Nezami A, Reynolds J, Alvi K, Goulet L, Stamos D. Ernst JT, et al. Among authors: nezami a. J Med Chem. 2014 Apr 24;57(8):3382-400. doi: 10.1021/jm500042s. Epub 2014 Apr 10. J Med Chem. 2014. PMID: 24673104
Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.
Clark MP, Ledeboer MW, Davies I, Byrn RA, Jones SM, Perola E, Tsai A, Jacobs M, Nti-Addae K, Bandarage UK, Boyd MJ, Bethiel RS, Court JJ, Deng H, Duffy JP, Dorsch WA, Farmer LJ, Gao H, Gu W, Jackson K, Jacobs DH, Kennedy JM, Ledford B, Liang J, Maltais F, Murcko M, Wang T, Wannamaker MW, Bennett HB, Leeman JR, McNeil C, Taylor WP, Memmott C, Jiang M, Rijnbrand R, Bral C, Germann U, Nezami A, Zhang Y, Salituro FG, Bennani YL, Charifson PS. Clark MP, et al. Among authors: nezami a. J Med Chem. 2014 Aug 14;57(15):6668-78. doi: 10.1021/jm5007275. Epub 2014 Jul 24. J Med Chem. 2014. PMID: 25019388
Preclinical activity of VX-787, a first-in-class, orally bioavailable inhibitor of the influenza virus polymerase PB2 subunit.
Byrn RA, Jones SM, Bennett HB, Bral C, Clark MP, Jacobs MD, Kwong AD, Ledeboer MW, Leeman JR, McNeil CF, Murcko MA, Nezami A, Perola E, Rijnbrand R, Saxena K, Tsai AW, Zhou Y, Charifson PS. Byrn RA, et al. Among authors: nezami a. Antimicrob Agents Chemother. 2015 Mar;59(3):1569-82. doi: 10.1128/AAC.04623-14. Epub 2014 Dec 29. Antimicrob Agents Chemother. 2015. PMID: 25547360 Free PMC article.
Isothermal titration calorimetry.
Velázquez-Campoy A, Ohtaka H, Nezami A, Muzammil S, Freire E. Velázquez-Campoy A, et al. Among authors: nezami a. Curr Protoc Cell Biol. 2004 Sep;Chapter 17:Unit 17.8. doi: 10.1002/0471143030.cb1708s23. Curr Protoc Cell Biol. 2004. PMID: 18228446 Review.
45 results