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

BMX (P51813) - Overview - Molecular Target Synopsis

Protein


BMX, Cytoplasmic tyrosine-protein kinase BMX
Enzyme Classification 2.7.10.2
UniProt P51813

Also Known as BMX_HUMAN, BMX

Non-receptor tyrosine kinase that plays central but diverse modulatory roles in various signaling processes involved in the regulation of actin reorganization, cell migration, cell proliferation and survival, cell adhesion, and apoptosis. Participates in signal transduction stimulated by growth factor receptors, cytokine receptors, G-protein coupled receptors, antigen receptors and integrins. Induces tyrosine phosphorylation of BCAR1 in response to integrin regulation. Activation of BMX by integrins is mediated by PTK2/FAK1, a key mediator of integrin signaling events leading to the regulation of actin cytoskeleton and cell motility. Plays a critical role in TNF-induced angiogenesis, and implicated in the signaling of TEK and FLT1 receptors, 2 important receptor families essential for angiogenesis. Required for the phosphorylation and activation of STAT3, a transcription factor involved in cell differentiation. Also involved in interleukin-6 (IL6) induced differentiation. Plays also a role in programming adaptive cytoprotection against extracellular stress in different cell systems, salivary epithelial cells, brain endothelial cells, and dermal fibroblasts. May be involved in regulation of endocytosis through its interaction with an endosomal protein RUFY1. May also play a role in the growth and differentiation of hematopoietic cells; as well as in signal transduction in endocardial and arterial endothelial cells. Interacts with BCAR1, CAV1, MYD88, PTK2/FAK1, RUFY1, RUFY2, STAT3, TIRAP and TNFRSF1B.

3SXR
CRYSTAL STRUCTURE OF BMX NON-RECEPTOR TYROSINE KINASE COMPLEX WITH DASATINIB
RCSB/PDB
Inspect Structure
See all 3D Structures for BMX

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
675ENSG00000102010ENST00000348343, ENST00000357607, ENST00000342014ENSP00000308774, ENSP00000350224, ENSP00000340082P51813-1

Sub-cellular localization


UniProt: BMX is active in the following subcellular-locations: cytoplasm.
GO terms: BMX is active in the following subcellular-locations: cytosol, nucleoplasm, plasma membrane, ruffle membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project BMX has gain in 0 cell-lines, loss in 52 cell-lines and no signal in 953 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SK_MEL_2, K_562, MCF7

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SK-MEL-2, HCC1482, KARPAS-422

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: HUVEC, SK-N-SH, NHLF

(see details)

RNA Interference


BMX was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: SKOV3, SMOV2. (see details)

3D Structures


For BMX there are:
4 structures (5 chains) solved
2 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

BMX is solved in complex with the approved drug(s):

1N1/DASATINIB (3SXR_A, 3SXR_B).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


BMX has been screened with 758 compounds (1404 bioactivities), 28 compounds have bioactivities that show binding affinity of <= 500nM (39 bioactivities). (see details)