Identification of potential small molecule binding pockets on Rho family GTPases.

ABSTRACT: Rho GTPases are conformational switches that control a wide variety of signaling pathways critical for eukaryotic cell development and proliferation. They represent attractive targets for drug design as their aberrant function and deregulated activity is associated with many human diseases including cancer. Extensive high-resolution structures (>100) and recent mutagenesis studies have laid the foundation for the design of new structure-based chemotherapeutic strategies. Although the inhibition of Rho signaling with drug-like compounds is an active area of current research, very little attention has been devoted to directly inhibiting Rho by targeting potential allosteric non-nucleotide binding sites. By avoiding the nucleotide binding site, compounds may minimize the potential for undesir

SUBMITTER: Ortiz-Sanchez JM 

PROVIDER: S-EPMC3397943 | biostudies-literature | 2012

REPOSITORIES: biostudies-literature