Rho GTPase-activating protein 1 (ARHGAP1)

Rho GTPase-activating protein 1 (ARHGAP1) is an enzyme that belongs to the RhoGAP family and functions as a negative regulator of Rho family small GTPases, including CDC42 and RhoA[2][3]. By stimulating the intrinsic GTPase activity of these signaling proteins, ARHGAP1 converts them from an active GTP-bound form to an inactive GDP-bound form, thereby downregulating pathways involved in actin cytoskeleton organization, cell migration, invasion, and cell proliferation[2][1][3]. Evidence suggests that ARHGAP1 exhibits tumor suppressor activity: its overexpression inhibits cancer cell proliferation, migration, and invasion, while lower expression levels are correlated with larger tumors and higher invasiveness, particularly in cancers such as cervical carcinoma and breast cancer[1]. ARHGAP1 operates as part of complex signaling pathways, and its activity and specificity to different Rho GTPases can be further regulated by associated domains and subcellular localization[2][3]. Note: No drugs directly targeting ARHGAP1 are reported in the search results. Its involvement is more as a signaling regulator and potential biomarker/tumor suppressor than a direct drug target at present.

Other names

RhoGAPCDC42GAPRhoGAP1p50rhoGAPCdc42GAPrho GTPase-activating protein 1GTPase-activating protein rhoGAPGTPase-activating protein, Rho, 1Rho-related small GTPase protein activatorRho-type GTPase-activating protein 1p50-RhoGAP

Inhibition of Rho and CDC42 GTPase activity by promoting GTP hydrolysis (resulting in inactivation of these signaling proteins)[1][2][3]