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Selective inhibition of biotin protein ligase from Staphylococcus aureus.


ABSTRACT: There is a well documented need to replenish the antibiotic pipeline with new agents to combat the rise of drug resistant bacteria. One strategy to combat resistance is to discover new chemical classes immune to current resistance mechanisms that inhibit essential metabolic enzymes. Many of the obvious drug targets that have no homologous isozyme in the human host have now been investigated. Bacterial drug targets that have a closely related human homologue represent a new frontier in antibiotic discovery. However, to avoid potential toxicity to the host, these inhibitors must have very high selectivity for the bacterial enzyme over the human homolog. We have demonstrated that the essential enzyme biotin protein ligase (BPL) from the clinically important pathogen Staphylococcus aureus coul

SUBMITTER: Soares da Costa TP 

PROVIDER: S-EPMC3366794 | biostudies-literature | 2012 May

REPOSITORIES: biostudies-literature