bone morphogenetic protein receptor type 2 | Type II receptor serine/threonine kinases | IUPHAR/BPS Guide to PHARMACOLOGY

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bone morphogenetic protein receptor type 2

Target not currently curated in GtoImmuPdb

Target id: 1794

Nomenclature: bone morphogenetic protein receptor type 2

Abbreviated Name: BMPR2

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
Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1038 2q33-q34 BMPR2 bone morphogenetic protein receptor type 2
Mouse 1 1038 1 C2 Bmpr2 bone morphogenetic protein receptor, type II (serine/threonine kinase)
Rat - 1038 9q31 Bmpr2 bone morphogenetic protein receptor type 2
Previous and Unofficial Names
primary pulmonary hypertension 1 | bone morphogenetic protein receptor type-2 | BMPRII | BMP type II receptor | BMPR-2 | BMP receptor 2 | BMPR3 | BRK-3 | PPH1 | T-ALK | bone morphogenetic protein receptor, type II (serine/threonine kinase) | bone morphogenetic protein receptor
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of the Extracellular Domain of the Type II BMP Receptor
PDB Id:  2HLQ
Resolution:  1.45Å
Species:  Human
References:  4
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the kinase domain of bone morphogenetic protein receptor type II (BMPR2) at 2.35 A resolution
PDB Id:  3G2F
Resolution:  2.35Å
Species:  Human
References: 
Enzyme Reaction
EC Number: 2.7.11.30
Natural/Endogenous Ligands
Comments: Endogenous ligands may include growth/differentiation factor-6 [1].

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

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 13a [PMID: 23639540] Hs Inhibition 7.8 pIC50 3
pIC50 7.8 (IC50 1.59x10-8 M) [3]
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: 2,5

Key to terms and symbols Click column headers to sort
Target used in screen: BMPR2
Ligand Sp. Type Action Value Parameter
PP-242 Hs Inhibitor Inhibition 7.1 pKd
SU-14813 Hs Inhibitor Inhibition 6.7 pKd
JNJ-28312141 Hs Inhibitor Inhibition 6.5 pKd
KW-2449 Hs Inhibitor Inhibition 6.4 pKd
sunitinib Hs Inhibitor Inhibition 6.2 pKd
bosutinib Hs Inhibitor Inhibition 6.2 pKd
ruxolitinib Hs Inhibitor Inhibition 6.0 pKd
lestaurtinib Hs Inhibitor Inhibition 5.8 pKd
staurosporine Hs Inhibitor Inhibition 5.6 pKd
fedratinib Hs Inhibitor Inhibition 5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
Disease:  Pulmonary hypertension, primary, 1; PPH1
Synonyms: Heritable pulmonary arterial hypertension [Orphanet: ORPHA275777]
Idiopathic pulmonary arterial hypertension [Orphanet: ORPHA275766]
Primary pulmonary hypertension [Disease Ontology: DOID:14557]
Disease Ontology: DOID:14557
OMIM: 178600
Orphanet: ORPHA275777, ORPHA275766
Disease:  Pulmonary venoocclusive disease 1, autosomal dominant; PVOD1
Synonyms: Pulmonary venoocclusive disease [Orphanet: ORPHA31837] [Disease Ontology: DOID:5453]
Disease Ontology: DOID:5453
OMIM: 265450
Orphanet: ORPHA31837

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. 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. Engers DW, Frist AY, Lindsley CW, Hong CC, Hopkins CR. (2013) Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe. Bioorg. Med. Chem. Lett., 23 (11): 3248-52. [PMID:23639540]

4. Mace PD, Cutfield JF, Cutfield SM. (2006) High resolution structures of the bone morphogenetic protein type II receptor in two crystal forms: implications for ligand binding. Biochem. Biophys. Res. Commun., 351 (4): 831-8. [PMID:17094948]

5. 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: bone morphogenetic protein receptor type 2. Last modified on 29/01/2016. Accessed on 22/08/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1794.