Target intelligence / Profile preview

BCR-ABL tyrosine kinase (BCR-ABL)

Target
BCR-ABL
Molecular classification
Enzyme, Tyrosine kinase, Non-receptor tyrosine kinase
01

Overview

The BCR-ABL tyrosine kinase is a fusion protein resulting from a reciprocal translocation between chromosomes 9 and 22, creating what is known as the Philadelphia chromosome. This genetic abnormality leads to the fusion of the BCR and ABL1 genes, producing a constitutively active tyrosine kinase that drives the development of chronic myelogenous leukemia. The protein functions as a non-receptor tyrosine kinase that phosphorylates various substrate proteins, activating multiple signaling pathways that promote cell proliferation and survival. The development of tyrosine kinase inhibitors targeting BCR-ABL has revolutionized the treatment of CML, transforming it from a fatal disease to a manageable chronic condition for many patients.

Other names
Philadelphia chromosome proteinp210 BCR-ABL
02

Mechanism of action

Tyrosine kinase inhibition, ATP-competitive binding, Inhibition of BCR-ABL autophosphorylation

03

Biological functions

Cell growth regulationCell survivalCytoskeleton remodelingSignal transductionCell proliferation
04

Disease associations

CancerChronic myelogenous leukemia (CML)
05

Safety considerations

Development of resistance mutations (especially T315I)Drug intolerance
06

Interacting drugs

2 more in the full profile.

07

Biomarkers

BCR-ABL expressionT315I mutation status

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