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Target intelligence / Profile preview
Rho GTPase activating protein 5 (ARHGAP5)
- Target
- ARHGAP5
- Molecular classification
- Enzyme, Rho GTPase-activating protein, Signal transduction regulator
01
Overview
Rho GTPase activating protein 5 (ARHGAP5) is an enzyme that functions as a GTPase-activating protein (GAP) primarily for Rho family GTPases such as RhoA, negatively regulating their activity by accelerating GTP hydrolysis. It is a key regulator of cytoskeletal dynamics, cell migration, and invasion, and plays a crucial role in processes such as epithelial-mesenchymal transition. Overexpression of ARHGAP5 has been implicated in increased metastatic potential of cancers (including colorectal, lung, and liver cancers) and is associated with poor clinical prognosis. Genetic variants in ARHGAP5 have been implicated in autism spectrum disorder, reflecting its importance in neurological development. ARHGAP5 is regulated at the transcriptional and post-transcriptional levels by factors such as CREB1 and microRNAs[1][2][3].
- Other names
- ARHGAP5RhoGAP5p190-Bp190BRhoGAPGFI2growth factor independent 2p105 RhoGAPp100 RasGAP-associated p105 proteinrho-type GTPase-activating protein 5
02
Mechanism of action
Inhibits RhoA and other Rho GTPases by stimulating the hydrolysis of GTP to GDP, thus inactivating these signaling molecules
03
Biological functions
Negative regulation of Rho GTPasesCytoskeleton organizationRegulation of cell migration and invasionEpithelial-mesenchymal transition (EMT)Signal transduction
04
Disease associations
Cancer (lung cancer, colorectal cancer, hepatocellular carcinoma, gastric cancer)Autism spectrum disorderOther (Martsolf syndrome 1)
05
Safety considerations
As a target, its role in normal cytoskeletal dynamics poses potential risk for adverse effects on normal cell migration and tissue homeostasis if inhibited
06
Biomarkers
Increased ARHGAP5 expression is associated with metastatic potential and poor prognosis in colorectal cancerARHGAP5 gene variants linked to autism spectrum disorder
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