Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

ACVR2A (P27037) - Overview - Molecular Target Synopsis

Protein


ACVR2A, Activin receptor type-2A
Enzyme Classification 2.7.11.30
UniProt P27037

Also Known as AVR2A_HUMAN, ACVR2A, ACVR2

On ligand binding, forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. Type II receptors phosphorylate and activate type I receptors which autophosphorylate, then bind and activate SMAD transcriptional regulators. Receptor for activin A, activin B and inhibin A. Mediates induction of adipogenesis by GDF6. Interacts with AIP1. Part of a complex consisting of AIP1, ACVR2A, ACVR1B and SMAD3.

5NH3
CRYSTAL STRUCTURE OF THE ACTIVIN RECEPTOR TYPE-2A LIGAND BINDING DOMAIN IN COMPLEX WITH BIMAGRUMAB FV
RCSB/PDB
Inspect Structure
See all 3D Structures for ACVR2A

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
513ENSG00000121989ENST00000241416, ENST00000404590ENSP00000241416, ENSP00000384338P27037-1
405ENSG00000121989ENST00000535787ENSP00000439988P27037-2

Sub-cellular localization


UniProt: ACVR2A is active in the following subcellular-locations: membrane.
GO terms: ACVR2A is active in the following subcellular-locations: activin receptor complex, cell surface, cytoplasm, inhibin-betaglycan-ActRII complex, integral component of plasma membrane, plasma membrane, receptor complex.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project ACVR2A has gain in 0 cell-lines, loss in 3 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: OVCAR_5, IGROV1, HS578T

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H345, DMS 79, NCI-H847

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: SK-N-SH, A549, HMEC

(see details)

RNA Interference


ACVR2A was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: MCF12A, PL5. (see details)

3D Structures


For ACVR2A there are:
4 structures (8 chains) solved
4 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


ACVR2A has been screened with 101 compounds (139 bioactivities), 4 compounds have bioactivities that show binding affinity of <= 500nM (5 bioactivities). (see details)