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Murgocil is a highly bioactive staphylococcal-specific inhibitor of the peptidoglycan glycosyltransferase enzyme MurG.
Mann PA, Müller A, Xiao L, Pereira PM, Yang C, Ho Lee S, Wang H, Trzeciak J, Schneeweis J, Dos Santos MM, Murgolo N, She X, Gill C, Balibar CJ, Labroli M, Su J, Flattery A, Sherborne B, Maier R, Tan CM, Black T, Onder K, Kargman S, Monsma FJ Jr, Pinho MG, Schneider T, Roemer T. Mann PA, et al. Among authors: yang c. ACS Chem Biol. 2013 Nov 15;8(11):2442-51. doi: 10.1021/cb400487f. Epub 2013 Sep 5. ACS Chem Biol. 2013. PMID: 23957438
TarO-specific inhibitors of wall teichoic acid biosynthesis restore β-lactam efficacy against methicillin-resistant staphylococci.
Lee SH, Wang H, Labroli M, Koseoglu S, Zuck P, Mayhood T, Gill C, Mann P, Sher X, Ha S, Yang SW, Mandal M, Yang C, Liang L, Tan Z, Tawa P, Hou Y, Kuvelkar R, DeVito K, Wen X, Xiao J, Batchlett M, Balibar CJ, Liu J, Xiao J, Murgolo N, Garlisi CG, Sheth PR, Flattery A, Su J, Tan C, Roemer T. Lee SH, et al. Among authors: yang c, yang sw. Sci Transl Med. 2016 Mar 9;8(329):329ra32. doi: 10.1126/scitranslmed.aad7364. Sci Transl Med. 2016. PMID: 26962156
Discovery of potent wall teichoic acid early stage inhibitors.
Labroli MA, Caldwell JP, Yang C, Lee SH, Wang H, Koseoglu S, Mann P, Yang SW, Xiao J, Garlisi CG, Tan C, Roemer T, Su J. Labroli MA, et al. Among authors: yang c, yang sw. Bioorg Med Chem Lett. 2016 Aug 15;26(16):3999-4002. doi: 10.1016/j.bmcl.2016.06.090. Epub 2016 Jun 30. Bioorg Med Chem Lett. 2016. PMID: 27436582
Can We Make Small Molecules Lean? Optimization of a Highly Lipophilic TarO Inhibitor.
Mandal M, Tan Z, Madsen-Duggan C, Buevich AV, Caldwell JP, Dejesus R, Flattery A, Garlisi CG, Gill C, Ha SN, Ho G, Koseoglu S, Labroli M, Basu K, Lee SH, Liang L, Liu J, Mayhood T, McGuinness D, McLaren DG, Wen X, Parmee E, Rindgen D, Roemer T, Sheth P, Tawa P, Tata J, Yang C, Yang SW, Xiao L, Wang H, Tan C, Tang H, Walsh P, Walsh E, Wu J, Su J. Mandal M, et al. Among authors: yang c, yang sw. J Med Chem. 2017 May 11;60(9):3851-3865. doi: 10.1021/acs.jmedchem.7b00113. Epub 2017 Mar 29. J Med Chem. 2017. PMID: 28322556
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: yang c, yang sw. 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
Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists.
Yang C, Balsells J, Chu HD, Cox JM, Crespo A, Ma X, Contino L, Brown P, Gao S, Zamlynny B, Wiltsie J, Clemas J, Lisnock J, Gibson J, Zhou G, Garcia-Calvo M, Bateman TJ, Tong V, Xu L, Crook M, Sinclair P, Shen HC. Yang C, et al. ACS Med Chem Lett. 2015 Mar 6;6(4):461-5. doi: 10.1021/acsmedchemlett.5b00010. eCollection 2015 Apr 9. ACS Med Chem Lett. 2015. PMID: 25941555 Free PMC article.
Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series.
Cox JM, Chu HD, Yang C, Shen HC, Wu Z, Balsells J, Crespo A, Brown P, Zamlynny B, Wiltsie J, Clemas J, Gibson J, Contino L, Lisnock J, Zhou G, Garcia-Calvo M, Bateman T, Xu L, Tong X, Crook M, Sinclair P. Cox JM, et al. Among authors: yang c. Bioorg Med Chem Lett. 2014 Apr 1;24(7):1681-4. doi: 10.1016/j.bmcl.2014.02.057. Epub 2014 Mar 1. Bioorg Med Chem Lett. 2014. PMID: 24630411
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.
Yang C, Shen HC, Wu Z, Chu HD, Cox JM, Balsells J, Crespo A, Brown P, Zamlynny B, Wiltsie J, Clemas J, Gibson J, Contino L, Lisnock J, Zhou G, Garcia-Calvo M, Bateman T, Xu L, Tong X, Crook M, Sinclair P. Yang C, et al. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4388-92. doi: 10.1016/j.bmcl.2013.05.077. Epub 2013 Jun 4. Bioorg Med Chem Lett. 2013. PMID: 23777778
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