Development of tag-free photoprobes for studies aimed at identifying the target of novel Group A Streptococcus antivirulence agents.

ABSTRACT: We previously reported the identification and development of novel inhibitors of streptokinase (SK) expression by Group A Streptococcus (GAS), originating from a high throughput cell-based phenotypic screen. Although phenotypic screening is well-suited to identifying compounds that exert desired biological effects in potentially novel ways, it requires follow-up experiments to determine the macromolecular target(s) of active compounds. We therefore designed and synthesized several classes of chemical probes for target identification studies, guided by previously established structure-activity relationships. The probes were designed to first irreversibly photolabel target proteins in the intact bacteria, followed by cell lysis and click ligation with fluorescent tags to allow for visualizat

SUBMITTER: Yestrepsky BD 

PROVIDER: S-EPMC4005860 | biostudies-literature | 2014 Mar

REPOSITORIES: biostudies-literature