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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: black ta. PLoS One. 2017 Jul 10;12(7):e0180965. doi: 10.1371/journal.pone.0180965. eCollection 2017. PLoS One. 2017. PMID: 28700746 Free PMC article.
Inhibitor of intramembrane protease RseP blocks the σE response causing lethal accumulation of unfolded outer membrane proteins.
Konovalova A, Grabowicz M, Balibar CJ, Malinverni JC, Painter RE, Riley D, Mann PA, Wang H, Garlisi CG, Sherborne B, Rigel NW, Ricci DP, Black TA, Roemer T, Silhavy TJ, Walker SS. Konovalova A, et al. Among authors: black ta. Proc Natl Acad Sci U S A. 2018 Jul 10;115(28):E6614-E6621. doi: 10.1073/pnas.1806107115. Epub 2018 Jun 25. Proc Natl Acad Sci U S A. 2018. PMID: 29941590 Free PMC article.
A small-molecule inhibitor of BamA impervious to efflux and the outer membrane permeability barrier.
Hart EM, Mitchell AM, Konovalova A, Grabowicz M, Sheng J, Han X, Rodriguez-Rivera FP, Schwaid AG, Malinverni JC, Balibar CJ, Bodea S, Si Q, Wang H, Homsher MF, Painter RE, Ogawa AK, Sutterlin H, Roemer T, Black TA, Rothman DM, Walker SS, Silhavy TJ. Hart EM, et al. Among authors: black ta. Proc Natl Acad Sci U S A. 2019 Oct 22;116(43):21748-21757. doi: 10.1073/pnas.1912345116. Epub 2019 Oct 7. Proc Natl Acad Sci U S A. 2019. PMID: 31591200 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. 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. 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
Discovery and optimization of antibacterial AccC inhibitors.
Cheng CC, Shipps GW Jr, Yang Z, Sun B, Kawahata N, Soucy KA, Soriano A, Orth P, Xiao L, Mann P, Black T. Cheng CC, et al. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6507-14. doi: 10.1016/j.bmcl.2009.10.057. Epub 2009 Oct 28. Bioorg Med Chem Lett. 2009. PMID: 19875284
Tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of left-hand-side moiety (Part-2).
Singh SB, Kaelin DE, Wu J, Miesel L, Tan CM, Black T, Nargund R, Meinke PT, Olsen DB, Lagrutta A, Lu J, Patel S, Rickert KW, Smith RF, Soisson S, Sherer E, Joyce LA, Wei C, Peng X, Wang X, Fukuda H, Kishii R, Takei M, Takano H, Shibasaki M, Yajima M, Nishimura A, Shibata T, Fukuda Y. Singh SB, et al. Bioorg Med Chem Lett. 2015 May 1;25(9):1831-5. doi: 10.1016/j.bmcl.2015.03.044. Epub 2015 Mar 24. Bioorg Med Chem Lett. 2015. PMID: 25851938
128 results