Target intelligence / Profile preview

Activin Type II Receptor (ActRII)

Target
ActRII
Molecular classification
Receptor, Transmembrane serine/threonine kinase, TGF-beta receptor family
01

Overview

Activin type II receptors (ActRIIA and ActRIIB) are transmembrane serine/threonine kinases belonging to the TGF-β receptor family. They play a crucial role in signal transduction for TGF-β ligands like activins, myostatin, and GDF11, influencing cell growth, differentiation, apoptosis, muscle mass regulation, and other processes. Upon ligand binding, they form heterotetrameric complexes with type I receptors, leading to Smad protein phosphorylation and gene expression modulation. Dysregulation is associated with diseases like myopathy and leukemia, making them therapeutic targets for muscle-wasting conditions and certain cancers.

Other names
Activin receptor type IIAACVR2AActivin A receptor type IIAActivin receptor type IIBACVR2BActivin A receptor type IIB
02

Mechanism of action

Ligand binding induces heterotetramer formation with type I receptors, followed by phosphorylation of Smad proteins and subsequent gene expression changes.

03

Biological functions

Cell growthCell differentiationHomeostasisOsteogenesisApoptosisMuscle mass regulationGene expression regulationSignal transduction
04

Disease associations

Idiopathic inflammatory myopathyAcute myeloid leukemiaMuscle wasting disordersCancer
05

Interacting drugs

Activin receptor inhibitors (e.g., antibodies against myostatin or ActRIIB)

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