Target intelligence / Profile preview

Transforming protein RhoA (Ras homolog family member A) (RhoA)

Target
RhoA
Molecular classification
Small GTPase, GTP-binding protein
01

Overview

Transforming protein RhoA (RhoA) is a small GTPase in the Rho family, encoded by the RHOA gene on chromosome 3. It cycles between inactive GDP-bound and active GTP-bound states, functioning as a molecular switch in signal transduction. Primarily regulates cytoskeleton dynamics, including actin polymerization, stress fiber formation, focal adhesions, and actomyosin contractility via effectors like ROCK1 and DIAPH1. Involved in cell migration, polarity, adhesion, cycle progression (G1 phase, cytokinesis), transcriptional control, and platelet activation. C-terminal prenylation anchors it to membranes; regulated by GEFs, GAPs, and GDIs. Overexpression promotes cancer progression; targeted for inhibition in cancer and nerve regeneration

Other names
Ras homolog family member AARH12ARHARho12RHOH12
02

Mechanism of action

Rho GTPase inhibition (prevents cell growth and proliferation)

03

Biological functions

Cytoskeleton organizationActin stress fiber formationActomyosin contractilityCell shape regulationCell migrationCell polarityCell cycle progressionTranscriptional controlSignal transduction
04

Disease associations

CancerCardiovascular disease (atherothrombolic stroke risk)AsthmaDiabetes
05

Safety considerations

Overexpression linked to tumor proliferation and metastasis; potential role in drug resistance (e.g., doxorubicin)
06

Interacting drugs

Rhosin
07

Biomarkers

RhoA protein expression (elevated in malignant prostate cancer, testicular tumors, associated with aggressiveness and metastasis)

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