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Page 1
Discovery and Optimization of Novel Pyrazolopyrimidines as Potent and Orally Bioavailable Allosteric HIV-1 Integrase Inhibitors.
Li G, Meanwell NA, Krystal MR, Langley DR, Naidu BN, Sivaprakasam P, Lewis H, Kish K, Khan JA, Ng A, Trainor GL, Cianci C, Dicker IB, Walker MA, Lin Z, Protack T, Discotto L, Jenkins S, Gerritz SW, Pendri A. Li G, et al. Among authors: gerritz sw. J Med Chem. 2020 Mar 12;63(5):2620-2637. doi: 10.1021/acs.jmedchem.9b01681. Epub 2020 Feb 21. J Med Chem. 2020. PMID: 32081010
Inhibition of influenza virus replication via small molecules that induce the formation of higher-order nucleoprotein oligomers.
Gerritz SW, Cianci C, Kim S, Pearce BC, Deminie C, Discotto L, McAuliffe B, Minassian BF, Shi S, Zhu S, Zhai W, Pendri A, Li G, Poss MA, Edavettal S, McDonnell PA, Lewis HA, Maskos K, Mörtl M, Kiefersauer R, Steinbacher S, Baldwin ET, Metzler W, Bryson J, Healy MD, Philip T, Zoeckler M, Schartman R, Sinz M, Leyva-Grado VH, Hoffmann HH, Langley DR, Meanwell NA, Krystal M. Gerritz SW, et al. Proc Natl Acad Sci U S A. 2011 Sep 13;108(37):15366-71. doi: 10.1073/pnas.1107906108. Epub 2011 Sep 6. Proc Natl Acad Sci U S A. 2011. PMID: 21896751 Free PMC article.
A novel small molecule inhibitor of hepatitis C virus entry.
Baldick CJ, Wichroski MJ, Pendri A, Walsh AW, Fang J, Mazzucco CE, Pokornowski KA, Rose RE, Eggers BJ, Hsu M, Zhai W, Zhai G, Gerritz SW, Poss MA, Meanwell NA, Cockett MI, Tenney DJ. Baldick CJ, et al. Among authors: gerritz sw. PLoS Pathog. 2010 Sep 2;6(9):e1001086. doi: 10.1371/journal.ppat.1001086. PLoS Pathog. 2010. PMID: 20838466 Free PMC article.
Small molecule receptor protein tyrosine phosphatase γ (RPTPγ) ligands that inhibit phosphatase activity via perturbation of the tryptophan-proline-aspartate (WPD) loop.
Sheriff S, Beno BR, Zhai W, Kostich WA, McDonnell PA, Kish K, Goldfarb V, Gao M, Kiefer SE, Yanchunas J, Huang Y, Shi S, Zhu S, Dzierba C, Bronson J, Macor JE, Appiah KK, Westphal RS, O'Connell J, Gerritz SW. Sheriff S, et al. Among authors: gerritz sw. J Med Chem. 2011 Oct 13;54(19):6548-62. doi: 10.1021/jm2003766. Epub 2011 Sep 20. J Med Chem. 2011. PMID: 21882820
Discovery of pyrazine carboxamide CB1 antagonists: the introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series.
Ellsworth BA, Wang Y, Zhu Y, Pendri A, Gerritz SW, Sun C, Carlson KE, Kang L, Baska RA, Yang Y, Huang Q, Burford NT, Cullen MJ, Johnghar S, Behnia K, Pelleymounter MA, Washburn WN, Ewing WR. Ellsworth BA, et al. Among authors: gerritz sw. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3978-82. doi: 10.1016/j.bmcl.2007.04.087. Epub 2007 Apr 29. Bioorg Med Chem Lett. 2007. PMID: 17513109
Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor.
Burford NT, Livingston KE, Canals M, Ryan MR, Budenholzer LM, Han Y, Shang Y, Herbst JJ, O'Connell J, Banks M, Zhang L, Filizola M, Bassoni DL, Wehrman TS, Christopoulos A, Traynor JR, Gerritz SW, Alt A. Burford NT, et al. Among authors: gerritz sw. J Med Chem. 2015 May 28;58(10):4220-9. doi: 10.1021/acs.jmedchem.5b00007. Epub 2015 May 7. J Med Chem. 2015. PMID: 25901762 Free PMC article.
34 results