Touchy-Feely Drug Design
Science · 2002
The active agent produced by Vibrio cholerae is cholera toxin, which contains five identical subunits arranged in the form of a pentagon. The toxin pentamer has been the target of studies aimed at designing prophylactic drugs for cholera. It can also serve as a model system for the design of inhibitor molecules that bind to several sites at the same time. If such multivalent inhibitors are optimized for interaction with the pentamer, they should exhibit higher affinity for the toxin than univalent or randomly oriented multivalent molecules.