High-throughput Screening of Small Molecule Inhibitors of the Streptococcus Quorum-sensing Signal Pathway.

ABSTRACT: The main components of the quorum-sensing system are expected to be favorable targets for drug development to combat various chronic infectious diseases. ComA of Streptococcus is an ATP-binding cassette transporter containing a peptidase domain (PEP), which is essential for the quorum-sensing signal production. Using high-throughput screening, we found a potent small molecule that suppressed the S. mutans quorum-sensing pathway through inhibition of PEP activity. The compound effectively attenuated the biofilm formation and competence development of S. mutans without inhibiting cell growth. The kinetic and structural studies with this molecule and a related compound unexpectedly revealed an allosteric site of PEP. This relatively hydrophobic site is thought to undergo large structural chan

SUBMITTER: Ishii S 

PROVIDER: S-EPMC5481443 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature