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Bacterial efflux transporters' polyspecificity - a gift and a curse?


ABSTRACT: All mechanisms of clinical antibiotic resistance benefit from activities of polyspecific efflux pumps acting to reduce intracellular accumulation of toxins and antibiotics. In Gram-negative bacteria, the major polyspecific efflux transporters belong to the Resistance-Nodulation-cell Division (RND) superfamily of proteins, which are capable of expelling thousands of structurally diverse compounds. Recent structural and functional advances generated novel insights into mechanisms underlying the biochemical versatility of RND transporters. This opinion article reviews these mechanisms and discusses implications of the polyspecificity of RND transporters for bacterial survival and for the development of efflux pump inhibitors effective in clinics.

SUBMITTER: Zgurskaya HI 

PROVIDER: S-EPMC8169617 | biostudies-literature | 2021 Jun

REPOSITORIES: biostudies-literature

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Bacterial efflux transporters' polyspecificity - a gift and a curse?

Zgurskaya Helen I HI   Malloci Giuliano G   Chandar Brinda B   Vargiu Attilio V AV   Ruggerone Paolo P  

Current opinion in microbiology 20210430


All mechanisms of clinical antibiotic resistance benefit from activities of polyspecific efflux pumps acting to reduce intracellular accumulation of toxins and antibiotics. In Gram-negative bacteria, the major polyspecific efflux transporters belong to the Resistance-Nodulation-cell Division (RND) superfamily of proteins, which are capable of expelling thousands of structurally diverse compounds. Recent structural and functional advances generated novel insights into mechanisms underlying the bi  ...[more]

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