Cancer Institute A national cancer institute
designated cancer center

Matthew Bogyo

Publication Details

  • Small molecule-induced allosteric activation of the Vibrio cholerae RTX cysteine protease domain SCIENCE Lupardus, P. J., Shen, A., Bogyo, M., Garcia, K. C. 2008; 322 (5899): 265-268

    Abstract:

    Vibrio cholerae RTX (repeats in toxin) is an actin-disrupting toxin that is autoprocessed by an internal cysteine protease domain (CPD). The RTX CPD is efficiently activated by the eukaryote-specific small molecule inositol hexakisphosphate (InsP6), and we present the 2.1 angstrom structure of the RTX CPD in complex with InsP6. InsP6 binds to a conserved basic cleft that is distant from the protease active site. Biochemical and kinetic analyses of CPD mutants indicate that InsP6 binding induces an allosteric switch that leads to the autoprocessing and intracellular release of toxin-effector domains.

    View details for DOI 10.1126/science.1162403

    View details for Web of Science ID 000259902300050

    View details for PubMedID 18845756

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