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Page 1
Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
Hecker SJ, Reddy KR, Totrov M, Hirst GC, Lomovskaya O, Griffith DC, King P, Tsivkovski R, Sun D, Sabet M, Tarazi Z, Clifton MC, Atkins K, Raymond A, Potts KT, Abendroth J, Boyer SH, Loutit JS, Morgan EE, Durso S, Dudley MN. Hecker SJ, et al. Among authors: hirst gc. J Med Chem. 2015 May 14;58(9):3682-92. doi: 10.1021/acs.jmedchem.5b00127. Epub 2015 Mar 17. J Med Chem. 2015. PMID: 25782055
Fragment-based discovery of JAK-2 inhibitors.
Antonysamy S, Hirst G, Park F, Sprengeler P, Stappenbeck F, Steensma R, Wilson M, Wong M. Antonysamy S, et al. Bioorg Med Chem Lett. 2009 Jan 1;19(1):279-82. doi: 10.1016/j.bmcl.2008.08.064. Epub 2008 Aug 22. Bioorg Med Chem Lett. 2009. PMID: 19019674
Discovery of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease.
Leonard KA, Madge LA, Krawczuk PJ, Wang A, Kreutter KD, Bacani GM, Chai W, Smith RC, Tichenor MS, Harris MC, Malaviya R, Seierstad M, Johnson ME, Venable JD, Kim S, Hirst GC, Mathur AS, Rao TS, Edwards JP, Rizzolio MC, Koudriakova T. Leonard KA, et al. Among authors: hirst gc. J Med Chem. 2020 Mar 26;63(6):2915-2929. doi: 10.1021/acs.jmedchem.9b01439. Epub 2020 Mar 16. J Med Chem. 2020. PMID: 32134643
Discovery of JNJ-64264681: A Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
Tichenor MS, Wiener JJM, Rao NL, Bacani GM, Wei J, Pooley Deckhut C, Barbay JK, Kreutter KD, Chang L, Clancy KW, Murrey HE, Wang W, Ahn K, Huber M, Rex E, Coe KJ, Wu J, Rui H, Sepassi K, Gaudiano M, Bekkers M, Cornelissen I, Packman K, Seierstad M, Xiouras C, Bembenek SD, Alexander R, Milligan C, Balasubramanian S, Lebsack AD, Venable JD, Philippar U, Edwards JP, Hirst G. Tichenor MS, et al. J Med Chem. 2022 Nov 10;65(21):14326-14336. doi: 10.1021/acs.jmedchem.2c01026. Epub 2022 Oct 31. J Med Chem. 2022. PMID: 36314537
Discovery of thienopyridines as Src-family selective Lck inhibitors.
Abbott L, Betschmann P, Burchat A, Calderwood DJ, Davis H, Hrnciar P, Hirst GC, Li B, Morytko M, Mullen K, Yang B. Abbott L, et al. Among authors: hirst gc. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1167-71. doi: 10.1016/j.bmcl.2006.12.035. Epub 2006 Dec 15. Bioorg Med Chem Lett. 2007. PMID: 17234410
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity. 1. Optimization of the agonist "trigger".
Aquino CJ, Armour DR, Berman JM, Birkemo LS, Carr RA, Croom DK, Dezube M, Dougherty RW Jr, Ervin GN, Grizzle MK, Head JE, Hirst GC, James MK, Johnson MF, Miller LJ, Queen KL, Rimele TJ, Smith DN, Sugg EE. Aquino CJ, et al. Among authors: hirst gc. J Med Chem. 1996 Jan 19;39(2):562-9. doi: 10.1021/jm950626d. J Med Chem. 1996. PMID: 8558528
Synthesis and activity of N-cyanoguanidine-piperazine P2X7 antagonists.
Betschmann P, Bettencourt B, Donnelly-Roberts D, Friedman M, George J, Hirst G, Josephsohn N, Konopacki D, Li B, Maull J, Morytko MJ, Moore NS, Namovic M, Rafferty P, Salmeron-Garcia JA, Tarcsa E, Wang L, Woller K. Betschmann P, et al. Bioorg Med Chem Lett. 2008 Jul 15;18(14):3848-51. doi: 10.1016/j.bmcl.2008.06.055. Epub 2008 Jun 20. Bioorg Med Chem Lett. 2008. PMID: 18595695
20 results