Article
Pyridylpiperazine-based allosteric inhibitors of RND-type multidrug efflux pumps.
Nature communications - 10 Jan 2022
Plé Coline, Tam Heng-Keat, Vieira Da Cruz Anais, Compagne Nina, Jiménez-Castellanos Juan-Carlos, Müller Reinke T, Pradel Elizabeth, Foong Wuen Ee, Malloci Giuliano, Ballée Alexia, Kirchner Moritz A, Moshfegh Parisa, Herledan Adrien, Herrmann Andrea, Deprez Benoit, Willand Nicolas, Vargiu Attilio Vittorio, Pos Klaas M, Flipo Marion, Hartkoorn Ruben C
Abstract excerpt
Efflux transporters of the RND family confer resistance to multiple antibiotics in Gram-negative bacteria. Here, we identify and chemically optimize pyridylpiperazine-based compounds that potentiate antibiotic activity in E. coli through inhibition of its primary RND transporter, AcrAB-TolC. Characterisation of resistant E. coli mutants and structural biology analyses indicate that the compounds bind to a unique...
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