Target intelligence / Profile preview

Rho GTPase-activating protein 30 (ARHGAP30)

Target
ARHGAP30
Molecular classification
Enzyme, GTPase-activating protein, Signal transduction protein
01

Overview

Rho GTPase-activating protein 30 (ARHGAP30) is an enzyme and member of the RhoGAP family that negatively regulates Rho GTPase signaling by promoting the hydrolysis of GTP, inactivating Rho proteins involved in actin cytoskeletal organization and cell adhesion[1][2][6]. In addition to its canonical GAP activity, ARHGAP30 acts as a multifunctional tumor suppressor, especially by binding p53 and the acetyltransferase p300 to promote acetylation and functional activation of p53 in a Rho-independent manner, which enhances p53-mediated cell cycle arrest and apoptosis[4]. Low ARHGAP30 expression or DNA methylation is consistently associated with poorer prognosis in several cancers, notably colorectal cancer and lung adenocarcinoma, highlighting its potential as a therapeutic target and biomarker[1][4][2]. No known direct drugs or inhibitors currently target ARHGAP30, but its modulation of p53 and GTPase signaling pathways makes it a potential candidate for intervention in oncology. Safety concerns focus on its broad role in controlling both cytoskeletal dynamics and tumor suppressor pathways.

Other names
Rho GTPase activating protein 30ARHGAP30FLJ00267Rho-type GTPase-activating protein 30rho GTPase-activating protein 30rho-type GTPase-activating protein 30
02

Mechanism of action

Enhancement of GTP hydrolysis on Rho GTPases (inactivation of Rho signaling); Promotion of p53 acetylation (p300-mediated) and tumor suppressor function, independently of Rho-GAP activity.

03

Biological functions

Regulation of Rho GTPase signalingNegative regulation of Rho GTPase activityRegulation of cytoskeletal organizationModulation of p53 acetylation and activationRegulation of cell proliferationRegulation of apoptosisCell adhesionActin cytoskeleton remodeling
04

Disease associations

CancerTumor progression and metastasisPrognostic biomarker (especially in colorectal cancer and lung adenocarcinoma)Possible role in metabolic regulation
05

Safety considerations

Loss of expression or DNA methylation associated with cancer progression and poor prognosis[1][4]Potential unwanted effect on p53 signaling if dysregulated
06

Biomarkers

ARHGAP30 expression (prognostic in colorectal cancer and lung adenocarcinoma)DNA methylation status of ARHGAP30 (prognostic in lung adenocarcinoma)

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