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activin A receptor type 2A

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Target id: 1791

Nomenclature: activin A receptor type 2A

Abbreviated Name: ActR2

Family: Type II receptor serine/threonine kinases

Contents:

Quaternary Structure: Complexes
Bone morphogenetic protein receptors
Growth/differentiation factor receptors
Activin receptors
Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 513 2q22.3-q23.1 ACVR2A activin A receptor type 2A
Mouse 1 513 2 28.38 cM Acvr2a activin receptor IIA
Rat 1 513 3q12 Acvr2a activin A receptor type 2A
Previous and Unofficial Names Click here for help
activin A receptor, type II | activin receptor IIA | ActRIIa | activin receptor 2A | ACVR2 | activin A receptor type IIA
Database Links Click here for help
Alphafold P27037 (Hs), P27038 (Mm), P38444 (Rn)
BRENDA 2.7.11.30
ChEMBL Target CHEMBL5616 (Hs)
Ensembl Gene ENSG00000121989 (Hs), ENSMUSG00000052155 (Mm), ENSRNOG00000005334 (Rn)
Entrez Gene 92 (Hs), 11480 (Mm), 29263 (Rn)
Human Protein Atlas ENSG00000121989 (Hs)
KEGG Enzyme 2.7.11.30
KEGG Gene hsa:92 (Hs), mmu:11480 (Mm), rno:29263 (Rn)
OMIM 102581 (Hs)
Pharos P27037 (Hs)
RefSeq Nucleotide NM_001616 (Hs), NM_007396 (Mm), NM_031571 (Rn)
RefSeq Protein NP_001607 (Hs), NP_031422 (Mm), NP_113759 (Rn)
UniProtKB P27037 (Hs), P27038 (Mm), P38444 (Rn)
Wikipedia ACVR2A (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of Activin receptor type-IIA (ACVR2A) kinase domain in complex with dorsomorphin
PDB Id:  3Q4T
Ligand:  dorsomorphin
Resolution:  1.96Å
Species:  Human
References: 
Enzyme Reaction Click here for help
EC Number: 2.7.11.30
Natural/Endogenous Ligands Click here for help
myostatin {Sp: Human}
Comments: Endogenous ligands may include growth/differentiation factor-6 [1].

Download all structure-activity data for this target as a CSV file go icon to follow link

Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
bimagrumab Peptide Click here for species-specific activity table Hs Binding 9.4 pKd 2
⤷ pKd 9.4 (Kd 4.34x10-10 M) [2]
Description: Binding affinity of clone MOR08159
DiscoveRx KINOMEscan® screen Click here for help
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 3-4
Key to terms and symbols Click column headers to sort
Target used in screen: ACVR2A
Ligand Sp. Type Action Value Parameter
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.0 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.7 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.5 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.7 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 5.6 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Immune regulation
Immuno Process:  Immune system development

References

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1. Asai-Coakwell M, March L, Dai XH, Duval M, Lopez I, French CR, Famulski J, De Baere E, Francis PJ, Sundaresan P et al.. (2013) Contribution of growth differentiation factor 6-dependent cell survival to early-onset retinal dystrophies. Hum Mol Genet, 22 (7): 1432-42. [PMID:23307924]

2. Berger C, Herrmann T, Lu C, Sheppard K-A, Trifilieff E, Urlinger S. (2013) Compositions and methods for increasing muscle growth. Patent number: US8388968. Assignee: Novartis Ag. Priority date: 27/04/2009. Publication date: 05/03/2013.

3. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1046-51. [PMID:22037378]

4. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem Biol, 17 (11): 1241-9. [PMID:21095574]

How to cite this page

Type II receptor serine/threonine kinases: activin A receptor type 2A. Last modified on 30/03/2016. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1791.