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activin A receptor type 2B

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Target not currently curated in GtoImmuPdb

Target id: 1792

Nomenclature: activin A receptor type 2B

Abbreviated Name: ActR2B

Family: Type II receptor serine/threonine kinases

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 1 512 3p22.2 ACVR2B activin A receptor type 2B
Mouse 1 536 9 F3 Acvr2b activin receptor IIB
Rat 1 513 8q32 Acvr2b activin A receptor type 2B
Previous and Unofficial Names Click here for help
activin receptor IIB | Activine receptor 2b (transmembrane serine kinase) | Acvr2 | activin receptor 2B | ActRIIB | activin A receptor type IIB
Database Links Click here for help
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of a ternary ligand-receptor complex of BMP-2 with ActR-IIB
PDB Id:  2H62
Resolution:  1.85Å
Species:  Human
References:  3
Enzyme Reaction Click here for help
EC Number: 2.7.11.30
Natural/Endogenous Ligands Click here for help
myostatin {Sp: Human}

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Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
bimagrumab Peptide Primary target of this compound Click here for species-specific activity table Hs Binding 11.8 pKd 1
pKd 11.8 (Kd 1.73x10-12 M) [1]
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: 2,4

Key to terms and symbols Click column headers to sort
Target used in screen: ACVR2B
Ligand Sp. Type Action Value Parameter
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.1 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.0 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.4 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.2 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 5.8 pKd
pazopanib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 5.6 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure 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
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Heterotaxy, visceral, 4, autosomal; HTX4
Synonyms: Situs ambiguus [Orphanet: ORPHA157769]
Visceral heterotaxy [Disease Ontology: DOID:0050545]
Disease Ontology: DOID:0050545
OMIM: 613751
Orphanet: ORPHA157769

References

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1. 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.

2. 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]

3. Weber D, Kotzsch A, Nickel J, Harth S, Seher A, Mueller U, Sebald W, Mueller TD. (2007) A silent H-bond can be mutationally activated for high-affinity interaction of BMP-2 and activin type IIB receptor. BMC Struct Biol, 7: 6. [PMID:17295905]

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 2B. Last modified on 30/03/2016. Accessed on 20/04/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1792.