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bone morphogenetic protein receptor type 2

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Target id: 1794

Nomenclature: bone morphogenetic protein receptor type 2

Abbreviated Name: BMPR2

Family: Type II receptor serine/threonine kinases

Contents:

Quaternary Structure: Complexes
Bone morphogenetic protein receptors
Growth/differentiation factor receptors
Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1038 2q33.1-q33.2 BMPR2 bone morphogenetic protein receptor type 2
Mouse 1 1038 1 C2 Bmpr2 bone morphogenetic protein receptor type 2
Rat - 1038 9q31 Bmpr2 bone morphogenetic protein receptor type 2
Previous and Unofficial Names Click here for help
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 Click here for help
Alphafold Q13873 (Hs), O35607 (Mm)
BRENDA 2.7.11.30
ChEMBL Target CHEMBL5467 (Hs)
Ensembl Gene ENSG00000204217 (Hs), ENSMUSG00000067336 (Mm), ENSRNOG00000022196 (Rn)
Entrez Gene 659 (Hs), 12168 (Mm), 140590 (Rn)
Human Protein Atlas ENSG00000204217 (Hs)
KEGG Enzyme 2.7.11.30
KEGG Gene hsa:659 (Hs), mmu:12168 (Mm), rno:140590 (Rn)
OMIM 600799 (Hs)
Orphanet ORPHA119057 (Hs)
Pharos Q13873 (Hs)
RefSeq Nucleotide NM_001204 (Hs), NM_007561 (Mm), NM_080407 (Rn)
RefSeq Protein NP_001195 (Hs), NP_031587 (Mm), NP_536332 (Rn)
UniProtKB Q13873 (Hs), O35607 (Mm)
Wikipedia BMPR2 (Hs)
Selected 3D Structures Click here for help
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 Click here for help
EC Number: 2.7.11.30
Natural/Endogenous Ligands Click here for help
Comments: Endogenous ligands may include growth/differentiation factor-6 [1].

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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] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.8 pIC50 3
⤷ pIC50 7.8 (IC50 1.59x10-8 M) [3]
deucravacitinib Small molecule or natural product Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.7 pIC50 6
⤷ pIC50 6.7 (IC50 1.93x10-7 M) [6]
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: 2,5
Key to terms and symbols Click column headers to sort
Target used in screen: BMPR2
Ligand Sp. Type Action Value Parameter
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.7 pKd
JNJ-28312141 Small molecule or natural product Hs Inhibitor Inhibition 6.5 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.4 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.2 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.0 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 5.8 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.6 pKd
fedratinib 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:  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]

6. Wrobleski ST, Moslin R, Lin S, Zhang Y, Spergel S, Kempson J, Tokarski JS, Strnad J, Zupa-Fernandez A, Cheng L et al.. (2019) Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165. J Med Chem, 62 (20): 8973-8995. [PMID:31318208]

Contributors

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