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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: labroli m. 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
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: labroli m. 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
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
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: labroli m. 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. Among authors: labroli m. Sci Transl Med. 2016 Mar 9;8(329):329ra32. doi: 10.1126/scitranslmed.aad7364. Sci Transl Med. 2016. PMID: 26962156
Chemical Genetic Analysis and Functional Characterization of Staphylococcal Wall Teichoic Acid 2-Epimerases Reveals Unconventional Antibiotic Drug Targets.
Mann PA, Müller A, Wolff KA, Fischmann T, Wang H, Reed P, Hou Y, Li W, Müller CE, Xiao J, Murgolo N, Sher X, Mayhood T, Sheth PR, Mirza A, Labroli M, Xiao L, McCoy M, Gill CJ, Pinho MG, Schneider T, Roemer T. Mann PA, et al. Among authors: labroli m. PLoS Pathog. 2016 May 4;12(5):e1005585. doi: 10.1371/journal.ppat.1005585. eCollection 2016 May. PLoS Pathog. 2016. PMID: 27144276 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: labroli m. ACS Chem Biol. 2013 Nov 15;8(11):2442-51. doi: 10.1021/cb400487f. Epub 2013 Sep 5. ACS Chem Biol. 2013. PMID: 23957438
22 results