activin A receptor type 2B | Type II receptor serine/threonine kinases | IUPHAR/BPS Guide to PHARMACOLOGY

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activin A receptor type 2B

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

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Quaternary Structure: Complexes
Bone morphogenetic protein receptors
Growth/differentiation factor receptors
Activin receptors
Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 512 3p22 ACVR2B activin A receptor type 2B
Mouse 1 536 9 Acvr2b activin receptor IIB
Rat 1 512 8q32 Acvr2b activin A receptor type 2B
Previous and Unofficial Names
activin receptor IIB | Activine receptor 2b (transmembrane serine kinase) | Acvr2 | activin receptor 2B | ActRIIB | activin A receptor type IIB
Database Links
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
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
EC Number: 2.7.11.30
Natural/Endogenous Ligands
myostatin {Sp: Human}

Download all structure-activity data for this target as a CSV file

Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
bimagrumab Hs Binding 11.8 pKd 1
pKd 11.8 (Kd 1.73x10-12 M) [1]
Description: Binding affinity of clone MOR08159
DiscoveRx KINOMEscan® screen
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 Hs Inhibitor Inhibition 8.1 pKd
PD-173955 Hs Inhibitor Inhibition 8.0 pKd
KW-2449 Hs Inhibitor Inhibition 6.4 pKd
dasatinib Hs Inhibitor Inhibition 6.2 pKd
AST-487 Hs Inhibitor Inhibition 5.8 pKd
pazopanib Hs Inhibitor Inhibition 5.6 pKd
alvocidib Hs Inhibitor Inhibition 5.6 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
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 11/07/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1792.