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Rapid Evolution of a Fragment-like Molecule to Pan-Metallo-Beta-Lactamase Inhibitors: Initial Leads toward Clinical Candidates.
Mandal M, Xiao L, Pan W, Scapin G, Li G, Tang H, Yang SW, Pan J, Root Y, de Jesus RK, Yang C, Prosise W, Dayananth P, Mirza A, Therien AG, Young K, Flattery A, Garlisi C, Zhang R, Chu D, Sheth P, Chu I, Wu J, Markgraf C, Kim HY, Painter R, Mayhood TW, DiNunzio E, Wyss DF, Buevich AV, Fischmann T, Pasternak A, Dong S, Hicks JD, Villafania A, Liang L, Murgolo N, Black T, Hagmann WK, Tata J, Parmee ER, Weber AE, Su J, Tang H. Mandal M, et al. Among authors: zhang r. J Med Chem. 2022 Dec 22;65(24):16234-16251. doi: 10.1021/acs.jmedchem.2c00766. Epub 2022 Dec 7. J Med Chem. 2022. PMID: 36475645
Selective small-molecule inhibition of an RNA structural element.
Howe JA, Wang H, Fischmann TO, Balibar CJ, Xiao L, Galgoci AM, Malinverni JC, Mayhood T, Villafania A, Nahvi A, Murgolo N, Barbieri CM, Mann PA, Carr D, Xia E, Zuck P, Riley D, Painter RE, Walker SS, Sherborne B, de Jesus R, Pan W, Plotkin MA, Wu J, Rindgen D, Cummings J, Garlisi CG, Zhang R, Sheth PR, Gill CJ, Tang H, Roemer T. Howe JA, et al. Among authors: zhang r. Nature. 2015 Oct 29;526(7575):672-7. doi: 10.1038/nature15542. Epub 2015 Sep 30. Nature. 2015. PMID: 26416753
Modulating the interaction between CDK2 and cyclin A with a quinoline-based inhibitor.
Deng Y, Shipps GW Jr, Zhao L, Siddiqui MA, Popovici-Muller J, Curran PJ, Duca JS, Hruza AW, Fischmann TO, Madison VS, Zhang R, McNemar CW, Mayhood TW, Syto R, Annis A, Kirschmeier P, Lees EM, Parry DA, Windsor WT. Deng Y, et al. Among authors: zhang r. Bioorg Med Chem Lett. 2014 Jan 1;24(1):199-203. doi: 10.1016/j.bmcl.2013.11.041. Epub 2013 Nov 23. Bioorg Med Chem Lett. 2014. PMID: 24332088
Lead Optimization to Advance Protease-Activated Receptor-1 Antagonists in Early Discovery.
Mandal M, Madeira M, Amin RP, Buevich AV, Cheng A, Labroli M, Liu X, Acton J, Pio B, Basso A, Chobanian H, Dong G, Dropinski J, Guo Y, Guo Z, Kurowski S, Korfmacher W, Lee S, Meng D, Ondeyka D, Yang Z, Zhang R, Wei H, Wu Z, Zhang F, Wollenberg G, Biftu T, Greenlee WJ, Chintala M, Maletic M, Zhu Z. Mandal M, et al. Among authors: zhang r, zhang f. J Med Chem. 2022 Apr 14;65(7):5575-5592. doi: 10.1021/acs.jmedchem.1c02048. Epub 2022 Mar 29. J Med Chem. 2022. PMID: 35349275
Catalytic activity of human ADAM33.
Zou J, Zhu F, Liu J, Wang W, Zhang R, Garlisi CG, Liu YH, Wang S, Shah H, Wan Y, Umland SP. Zou J, et al. Among authors: zhang r. J Biol Chem. 2004 Mar 12;279(11):9818-30. doi: 10.1074/jbc.M309696200. Epub 2003 Dec 15. J Biol Chem. 2004. PMID: 14676211 Free article.
Discovery of the HCV NS3/4A protease inhibitor (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3- [2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (Sch 503034) II. Key steps in structure-based optimization.
Prongay AJ, Guo Z, Yao N, Pichardo J, Fischmann T, Strickland C, Myers J Jr, Weber PC, Beyer BM, Ingram R, Hong Z, Prosise WW, Ramanathan L, Taremi SS, Yarosh-Tomaine T, Zhang R, Senior M, Yang RS, Malcolm B, Arasappan A, Bennett F, Bogen SL, Chen K, Jao E, Liu YT, Lovey RG, Saksena AK, Venkatraman S, Girijavallabhan V, Njoroge FG, Madison V. Prongay AJ, et al. Among authors: zhang r. J Med Chem. 2007 May 17;50(10):2310-8. doi: 10.1021/jm060173k. Epub 2007 Apr 20. J Med Chem. 2007. PMID: 17444623
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