Target intelligence / Profile preview

Ras p21 protein activator 2 (RASA2)

Target
RASA2
Molecular classification
Enzyme, GTPase-activating protein
01

Overview

Ras p21 protein activator 2 (RASA2, also known as GAP1M) is an enzyme and a member of the GAP1 family of GTPase-activating proteins[1][3]. RASA2 negatively regulates RAS proteins by stimulating their intrinsic GTPase activity, thereby converting active GTP-bound RAS to its inactive GDP-bound form. This action serves as a critical brake on RAS-mediated signal transduction, controlling key cellular processes such as proliferation and differentiation. RASA2 mutations or loss can promote aberrant RAS activation and are implicated in several diseases, including various cancers (e.g., melanoma, lung cancer) and genetic syndromes like Noonan syndrome and cardiofaciocutaneous syndrome. RASA2 also shows potential as a predictive biomarker for radiotherapy response in lung cancer, given that mutations in RASA2 can drive radioresistance by altering p53 function[1][2][3].

Other names
GAP1MRas GTPase-activating protein 2RasGAPGTPase-activating protein 1mGTPase-activating protein of RAS
02

Mechanism of action

Enhancement of RAS GTPase activity leading to RAS inactivation; drugs targeting this would likely act by modulating RAS-MAPK pathway activity

03

Biological functions

Signal transductionCell proliferationCell differentiation
04

Disease associations

CancerNoonan syndromeCardiofaciocutaneous syndromeTumor suppressionRadioresistance
05

Safety considerations

Potential loss of tumor suppressor function leading to cancer predispositionpossible side effects from modulating RAS pathway
06

Biomarkers

Predictive marker for radiotherapy response in lung cancer; the presence of mutated RASA2 may predict poor response to radiation therapy

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