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- W3177715446 abstract "MmpL3, an essential mycolate transporter in the inner membrane of Mycobacterium tuberculosis (Mtb), has been identified as a target of multiple, chemically diverse antitubercular drugs. However, several of these molecules seem to have secondary targets and inhibit bacterial growth by more than one mechanism. Here, we describe a cell-based assay that utilizes two-way regulation of MmpL3 expression to readily identify MmpL3-specific inhibitors. We successfully used this assay to identify a novel guanidine-based MmpL3 inhibitor from a library of 220 compounds that inhibit growth of Mtb by largely unknown mechanisms. We furthermore identified inhibitors of cytochrome bc1-aa3 oxidase as one class of off-target hits in whole-cell screens for MmpL3 inhibitors and report a novel sulfanylacetamide as a potential QcrB inhibitor." @default.
- W3177715446 created "2021-07-19" @default.
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- W3177715446 date "2020-12-15" @default.
- W3177715446 modified "2023-10-16" @default.
- W3177715446 title "Two-Way Regulation of MmpL3 Expression Identifies and Validates Inhibitors of MmpL3 Function in <i>Mycobacterium tuberculosis</i>" @default.
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- W3177715446 doi "https://doi.org/10.1021/acsinfecdis.0c00675" @default.
- W3177715446 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/7802072" @default.
- W3177715446 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/33319550" @default.
- W3177715446 hasPublicationYear "2020" @default.
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