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dc.contributor.authorYe, Jen_US
dc.contributor.authorChu, AJen_US
dc.contributor.authorLin, Len_US
dc.contributor.authorYang, Xen_US
dc.contributor.authorMa, Cen_US
dc.identifier.citationMolecules, 2019, v. 24, no. 16, 2902en_US
dc.description.abstractNovel antimicrobial classes are in desperate need for clinical management of infections caused by increasingly prevalent multi-drug resistant pathogens. The protein-protein interaction between bacterial RNA polymerase (RNAP) and the housekeeping sigma initiation factor is essential to transcription and bacterial viability. It also presents a potential target for antimicrobial discovery, for which a hit compound (C3) was previously identified from a pharmacophore modelbased in silico screen. In this study, the hit compound was experimentally assessed with some rationally designed derivatives for the antimicrobial activities, in particular against Streptococcus pneumoniae and other pathogens. One compound, C3-005, shows dramatically improved activity against pneumococci compared to C3. C3-005 also attenuates S. pneumoniae toxin production more strongly than existing classes of antibiotics tested. Here we demonstrate a newly validated antimicrobial agent to address an overlooked target in the hit-to-lead process, which may pave the way for further antimicrobial development.en_US
dc.description.sponsorshipDepartment of Applied Biology and Chemical Technologyen_US
dc.publisherMolecular Diversity Preservation International (MDPI)en_US
dc.rights© 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (
dc.rightsThe following publication Ye J, Chu AJ, Lin L, Yang X, Ma C. First-In-Class Inhibitors Targeting the Interaction between Bacterial RNA Polymerase and Sigma Initiation Factor Affect the Viability and Toxin Release of Streptococcus pneumoniae. Molecules. 2019; 24(16):2902, is available at
dc.subjectAntimicrobial discoveryen_US
dc.subjectRNA polymeraseen_US
dc.subjectSigma factoren_US
dc.titleFirst-in-class inhibitors targeting the interaction between bacterial RNA polymerase and sigma initiation factor affect the viability and toxin release of streptococcus pneumoniaeen_US
dc.typeJournal/Magazine Articleen_US
dc.description.validate201910 bcma-
Appears in Collections:Journal/Magazine Article
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