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Page 1
Antibacterial small molecules targeting the conserved TOPRIM domain of DNA gyrase.
Walker SS, Labroli M, Painter RE, Wiltsie J, Sherborne B, Murgolo N, Sher X, Mann P, Zuck P, Garlisi CG, Su J, Kargman S, Xiao L, Scapin G, Salowe S, Devito K, Sheth P, Buist N, Tan CM, Black TA, Roemer T. Walker SS, et al. Among authors: tan cm. PLoS One. 2017 Jul 10;12(7):e0180965. doi: 10.1371/journal.pone.0180965. eCollection 2017. PLoS One. 2017. PMID: 28700746 Free PMC article.
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. 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. 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. 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
In Vitro and In Vivo Characterization of the Novel Oxabicyclooctane-Linked Bacterial Topoisomerase Inhibitor AM-8722, a Selective, Potent Inhibitor of Bacterial DNA Gyrase.
Tan CM, Gill CJ, Wu J, Toussaint N, Yin J, Tsuchiya T, Garlisi CG, Kaelin D, Meinke PT, Miesel L, Olsen DB, Lagrutta A, Fukuda H, Kishii R, Takei M, Oohata K, Takeuchi T, Shibue T, Takano H, Nishimura A, Fukuda Y, Singh SB. Tan CM, et al. Antimicrob Agents Chemother. 2016 Jul 22;60(8):4830-9. doi: 10.1128/AAC.00619-16. Print 2016 Aug. Antimicrob Agents Chemother. 2016. PMID: 27246784 Free PMC article.
Discovery of wall teichoic acid inhibitors as potential anti-MRSA β-lactam combination agents.
Wang H, Gill CJ, Lee SH, Mann P, Zuck P, Meredith TC, Murgolo N, She X, Kales S, Liang L, Liu J, Wu J, Santa Maria J, Su J, Pan J, Hailey J, Mcguinness D, Tan CM, Flattery A, Walker S, Black T, Roemer T. Wang H, et al. Among authors: tan cm. Chem Biol. 2013 Feb 21;20(2):272-84. doi: 10.1016/j.chembiol.2012.11.013. Chem Biol. 2013. PMID: 23438756 Free PMC article.
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: tan cm. ACS Chem Biol. 2013 Nov 15;8(11):2442-51. doi: 10.1021/cb400487f. Epub 2013 Sep 5. ACS Chem Biol. 2013. PMID: 23957438
Hydroxy tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of RHS moiety (Part-3).
Singh SB, Kaelin DE, Wu J, Miesel L, Tan CM, Gill C, Black T, Nargund R, Meinke PT, Olsen DB, Lagrutta A, Wei C, Peng X, Wang X, Fukuda H, Kishii R, Takei M, Takeuchi T, Shibue T, Ohata K, Takano H, Ban S, Nishimura A, Fukuda Y. Singh SB, et al. Among authors: tan cm. Bioorg Med Chem Lett. 2015 Jun 15;25(12):2473-8. doi: 10.1016/j.bmcl.2015.04.063. Epub 2015 Apr 28. Bioorg Med Chem Lett. 2015. PMID: 25978963
201 results