Synthetic group A streptogramin antibiotics that overcome Vat resistance.

ABSTRACT: Natural products serve as chemical blueprints for most antibiotics in clinical use. The evolutionary process by which these molecules arise is inherently accompanied by the co-evolution of resistance mechanisms that shorten the clinical lifetime of any given class of antibiotics¹. Virginiamycin acetyltransferase (Vat) enzymes are resistance proteins that provide protection against streptogramins², potent antibiotics against Gram-positive bacteria that inhibit the bacterial ribosome³. Owing to the challenge of selectively modifying the chemically complex, 23-membered macrocyclic scaffold of group A streptogramins, analogues that overcome the resistance conferred by Vat enzymes have not been previously developed². Here we report the design, synthes

SUBMITTER: Li Q 

PROVIDER: S-EPMC7546582 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature