Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

BMPR2 (Q13873) - Overview - Molecular Target Synopsis

Protein


BMPR2, Bone morphogenetic protein receptor type-2
Enzyme Classification 2.7.11.30
UniProt Q13873

Also Known as BMPR2_HUMAN, BMPR2, PPH1

On ligand binding, forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. Type II receptors phosphorylate and activate type I receptors which autophosphorylate, then bind and activate SMAD transcriptional regulators. Binds to BMP7, BMP2 and, less efficiently, BMP4. Binding is weak but enhanced by the presence of type I receptors for BMPs. Mediates induction of adipogenesis by GDF6. Interacts with GDF5.

3G2F
CRYSTAL STRUCTURE OF THE KINASE DOMAIN OF BONE MORPHOGENETIC PROTEIN RECEPTOR TYPE II (BMPR2) AT 2.35 A RESOLUTION
RCSB/PDB
Inspect Structure
See all 3D Structures for BMPR2

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
1038ENSG00000204217ENST00000374580ENSP00000363708Q13873-1
530ENSG00000204217ENST00000374574ENSP00000363702Q13873-2

Sub-cellular localization


Gene Copy Number Variation


In COSMIC - Cell Lines Project BMPR2 has gain in 0 cell-lines, loss in 0 cell-lines and no signal in 1005 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MALME_3M, LOXIMVI, SF_539

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: 928 mel, AGS, 888

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: HSMM, NHLF, AG445

(see details)

RNA Interference


BMPR2 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: MDAMB134VI, SKGT4. (see details)

3D Structures


For BMPR2 there are:
3 structures (4 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


BMPR2 has been screened with 121 compounds (159 bioactivities), 9 compounds have bioactivities that show binding affinity of <= 500nM (10 bioactivities). (see details)