Article
Inhibition of protein-protein interactions: the discovery of druglike beta-catenin inhibitors by combining virtual and biophysical screening.
Proteins - 1 Jul 2006
Trosset Jean-Yves, Dalvit Claudio, Knapp Stefan, Fasolini Marina, Veronesi Marina, Mantegani Sergio, Gianellini Laura M, Catana Cornel, Sundström Michael, Stouten Pieter F W, Moll Jürgen K
Abstract excerpt
The interaction between beta-catenin and Tcf family members is crucial for the Wnt signal transduction pathway, which is commonly mutated in cancer. This interaction extends over a very large surface area (4800 A(2)), and inhibiting such interactions using low molecular weight inhibitors is a challenge. However, protein surfaces frequently contain "hot spots," small patches that are the main mediators of binding...
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