Target intelligence / Profile preview

Bone marrow kinase on the X chromosome (BMX)

Target
BMX
Molecular classification
Enzyme, Non-receptor tyrosine kinase, Tec family kinase
01

Overview

Bone marrow kinase on the X chromosome (BMX), also known as ETK, is a non-receptor tyrosine kinase belonging to the Tec family (UniProt P51813). It is expressed in various tissues, including hematopoietic cells, vascular endothelial cells, and epithelial cells, where it regulates signaling pathways involved in cell growth, survival, and migration (PubMed: 25601543). BMX is characterized by a Pleckstrin Homology (PH) domain that allows it to interact with phosphatidylinositol-3,4,5-trisphosphate (PIP3), linking it to the PI3K signaling pathway (NCBI Gene ID: 660). In oncology, BMX is frequently overexpressed in cancers such as prostate, breast, and glioblastoma, contributing to tumor progression, metastasis, and resistance to apoptosis (PubMed: 17401013). It also plays a role in inflammatory responses and cardiovascular remodeling, making it a versatile therapeutic target (PubMed: 21810431). While specific BMX inhibitors like BMX-IN-1 have been developed for research, several clinically approved multi-kinase inhibitors, such as Ibrutinib, also target BMX as an off-target effect (PubChem CID: 24822711). Targeting BMX offers a potential strategy to overcome drug resistance in various malignancies and manage chronic inflammatory conditions.

Other names
Epithelial and endothelial tyrosine kinaseETKBMX non-receptor tyrosine kinasePSCTK1Cytoplasmic tyrosine-protein kinase BMX
02

Mechanism of action

Inhibition of the ATP-binding site of the BMX tyrosine kinase domain, preventing downstream phosphorylation and signaling of pathways such as STAT3 and AKT.

03

Biological functions

Signal transductionCell proliferationCell migrationAngiogenesisApoptosis regulationCell differentiation
04

Disease associations

CancerInflammationCardiovascular disease
05

Safety considerations

Off-target inhibition of other Tec family kinasesPotential cardiovascular toxicityImmunomodulatory effects
06

Interacting drugs

Ibrutinib

4 more in the full profile.

07

Biomarkers

BMX protein expressionBMX mRNA levelsPhosphorylated BMX (p-BMX)

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