Target intelligence / Profile preview

Activin type II receptor A (ACVR2A)

Target
ACVR2A
Molecular classification
Receptor, Transmembrane serine/threonine kinase receptor, TGF-β receptor family member
01

Overview

Activin type II receptor A is a high-affinity transmembrane protein that binds activin A, activin B, inhibin A, and myostatin, recruiting and phosphorylating type I receptors (such as ALK4/ACVR1B), which then activate receptor-regulated Smad transcription factors, culminating in gene regulatory responses[1][2][3][6]. It modulates key cellular processes including muscle and bone development, cell proliferation, and apoptosis, and is clinically relevant in several cancers and in muscle wasting conditions, where it is actively pursued as a pharmacological target for drug development[1][2][4][7].

Other names
ActRIIAACVR2activin A receptor type IIAactivin receptor type-2A
02

Mechanism of action

Inhibition/blockade of activin and myostatin signaling via antagonists or neutralizing antibodies to increase muscle mass or halt disease progression; Modulation of Smad2/3 signaling pathway to influence gene expression and cellular responses

03

Biological functions

Signal transductionRegulation of cell growthCell differentiationHomeostasisOsteogenesisApoptosisMuscle growth regulationReproduction
04

Disease associations

Cancer (notably colorectal and prostate cancer)Muscle wasting (cachexia, sarcopenia)Cardiovascular disease (including heart failure)Possible roles in immune and renal diseases, and skeletal malfunctions
05

Safety considerations

Potential off-target effects due to involvement in multiple physiological processes (growth, differentiation, metabolism)Risk of abnormal cell proliferation or tumorigenesis when signaling is excessively inhibited or dysregulatedPossible cardiac effects due to role in calcium handling and heart failure
06

Interacting drugs

Bimagrumab

2 more in the full profile.

07

Biomarkers

Follistatin-like 3 levels (circulating ligand)Activin ligand concentrationsACVR2A gene mutation status (colorectal cancer)

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