Structural Mechanisms and Drug Discovery Prospects of Rho GTPases.

ABSTRACT: Rho GTPases regulate cellular morphology and dynamics, and some are key drivers of cancer progression. This superfamily offers attractive potential targets for therapeutic intervention, with RhoA, Rac1 and Cdc42 being prime examples. The challenges in developing agents that act on these signaling enzymes include the lack of obvious druggable pockets and their membrane-bound activities. However, progress in targeting the similar Ras protein is illuminating new strategies for specifically inhibiting oncogenic GTPases. The structures of multiple signaling and regulatory states of Rho proteins have been determined, and the post-translational modifications including acylation and phosphorylation points have been mapped and their functional effects examined. The development of inhibitors to prob

SUBMITTER: Smithers CC 

PROVIDER: S-EPMC4931675 | biostudies-literature | 2016 Jun

REPOSITORIES: biostudies-literature