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Microbial esterases and ester prodrugs: An unlikely marriage for combating antibiotic resistance.


ABSTRACT: The rise of antibiotic resistance necessitates the search for new platforms for drug development. Prodrugs are common tools for overcoming drawbacks typically associated with drug formulation and delivery, with ester prodrugs providing a classic strategy for masking polar alcohol and carboxylic acid functionalities and improving cell permeability. Ester prodrugs are normally designed to have simple ester groups, as they are expected to be cleaved and reactivated by a wide spectrum of cellular esterases. However, a number of pathogenic and commensal microbial esterases have been found to possess significant substrate specificity and can play an unexpected role in drug metabolism. Ester protection can also introduce antimicrobial properties into previously nontoxic drugs through alterations

SUBMITTER: Larsen EM 

PROVIDER: S-EPMC6377847 | biostudies-literature | 2019 Feb

REPOSITORIES: biostudies-literature