Site-Directed Mutagenesis Reveals Amino Acid Residues in the Escherichia coli RND Efflux Pump AcrB That Confer Macrolide Resistance

Antimicrobial Agents and Chemotherapy
2009.0

Abstract

The Escherichia coli AcrB efflux pump is a key RND-type multidrug resistance pump. This study aimed to identify nonaromatic residues in AcrB that determine macrolide resistance (MR). A hybrid AcrB-615-628MexB (replacing AcrB residues 615-628 with homologous MexB sequence) was constructed in an acrB-overexpressing E. coli strain. MIC assays showed the hybrid specifically reduced MR. Single mutations reintroduced into the hybrid revealed that AcrB residue 616 is critical: glycine (G616) confers MR, while asparagine (N616) (from MexB) reduces MR. Introducing G616N into wild-type AcrB reproduced the MR-sensitive phenotype, whereas I626M had no effect. Conclusion: AcrB position 616 determines MR level—G616 leads to macrolide resistance, N616 to sensitivity, with no impact on nonmacrolide antibiotics.

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