June 24, 2014
Researchers at the University of New Mexico have discovered a compound that is novel in that it is directly binding to the enzyme and prevents nucleotide binding.
Usually aberrant regulation or expression of Rho GTPases is linked to tumorigenesis or other disorders. For this reason the novel specific inhibitor of Cdc42 GTPase, capable of regulation of Rho GTPases activity, is extraordinarily useful, particularly since it is specific and acts reversibly. The identified novel small molecule specifically inhibits GTP binding to Cdc42. There are limited pharmacological tools targeting individual small GTPases, and most efforts have been focused on inhibiting post-translational GTPase modification by lipids, which is necessary for their membrane localization and activation.
During the past few years, Rho GTPases and their effector proteins have been recognized as major regulators of a wide range of signaling pathways that control various biological processes. Among different mammalian Rho GTPases, the most extensively characterized members are RhoA, Rac1, and Cdc42. Reorganization of the actin cytoskeleton is the most characterized function for Rho GTPases. Mammalian Rac1, Cdc42 and RhoA are implicated in lamellipodia, filopodia and stress fibers formation, respectively. Besides this, there is growing evidence that Rho-family GTPases are regulating cell-cycle progression, gene transcription, and have been implicated in cellular processes such as adhesion, migration, phagocytosis, cytokinesis, neurite extension and retraction, cellular morphogenesis and polarization, growth and cell survival. Despite the fact that Cdc42 specific inhibitors would be very useful and interesting for pharmacological use, up to date there is very little success in development of such drugs.
Researchers at the University of New Mexico have discovered a compound that is novel in that it is directly binding to the enzyme and prevents nucleotide binding. Usually aberrant regulation or expression of Rho GTPases is linked to tumorigenesis or other disorders. For this reason the novel specific inhibitor of Cdc42 GTPase, capable of regulation of Rho GTPases activity, is extraordinarily useful, particularly since it is specific and acts reversibly. The identified novel small molecule specifically inhibits GTP binding to Cdc42. There are limited pharmacological tools targeting individual small GTPases, and most efforts have been focused on inhibiting post-translational GTPase modification by lipids, which is necessary for their membrane localization and activation.
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stress fibers formation
regulating cell-cycle progression
filed intellectual property
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