Rho GTPase-activating protein 6 (ARHGAP6)

Rho GTPase-activating protein 6 (ARHGAP6) is an enzyme belonging to the RhoGAP family that regulates actin cytoskeleton dynamics by accelerating the intrinsic GTPase activity of Rho-type GTPases, primarily RhoA, thereby inactivating them[1][3][5]. ARHGAP6 has dual independent roles: one as a GTPase-activating protein affecting RhoA signaling and another as a cytoskeletal protein that binds actin filaments and promotes actin remodeling, process outgrowth, and changes in cell morphology. It is involved in key cellular functions such as motility and regulation of the actin cytoskeleton, and has been genetically linked to rare developmental disorders such as amelogenesis imperfecta and MLS syndrome[1][3][5]. No directly interacting drugs are currently documented or clinically validated for this target. Supporting details: ARHGAP6 is a protein-coding gene, and its protein product is a regulatory enzyme for RhoA-type GTPase signaling, which impacts actin cytoskeleton polymerization and cellular morphology[1][3][5]. It is distinguished by containing domains capable of both binding actin and acting as a GTPase-activator, giving it a unique dual function among cytoskeletal regulatory proteins[3][5]. Deficiency or deletion of ARHGAP6 is associated with the developmental disorder microphthalmia with linear skin defects (MLS) and amelogenesis imperfecta[1][3][5]. RHOGAPs as a family are important regulators in multiple cell processes (motility, growth, neural development), although no direct small molecule modulators or approved drugs are known for ARHGAP6 itself[4][2]. No documented clinical drug targeting ARHGAP6 exists; mechanisms of action relate to molecular inhibition of RhoA-type GTPase signaling[1][3][5].

Other names

Rho GTPase activating protein 6ARHGAP6RHOGAP6RhoGAPX-1Rho-type GTPase-activating protein 6Rho-type GTPase-activating protein RhoGAPX-1RHOGAPX-1rhoGAP6

Acceleration of GTP hydrolysis on RhoA-type GTPases, inactivating RhoA signaling[1][3][5]