Target intelligence / Profile preview

Breakpoint cluster region-Abelson murine leukemia viral oncogene homolog 1 fusion protein (BCR-ABL)

Target
BCR-ABL
Molecular classification
Tyrosine Kinase, Oncoprotein, Fusion Protein
01

Overview

The Breakpoint cluster region-Abelson murine leukemia viral oncogene homolog 1 fusion protein, commonly referred to as BCR-ABL, is a chimeric oncoprotein resulting from the fusion of the BCR gene (on chromosome 22) and the ABL1 gene (on chromosome 9). This hybrid protein exhibits constitutive tyrosine kinase activity, which drives abnormal cell proliferation. BCR-ABL is most famously associated with the Philadelphia chromosome, a hallmark of chronic myelogenous leukemia (CML) and some other leukemias. Several transcript variants exist, including p210 (most common in CML), p190 (more common in ALL), and p230 (a rare variant). Due to its role in driving leukemogenesis and the amenability to targeted treatment, BCR-ABL is a well-validated therapeutic target.

Other names
BCR–ABLPhiladelphia chromosome fusion protein
02

Mechanism of action

Inhibition of BCR-ABL tyrosine kinase activity

03

Biological functions

Cell proliferationCell cycle regulationSignal transductionTyrosine kinase activityLeukemogenesis
04

Disease associations

CancerChronic Myelogenous Leukemia (CML)Acute Lymphoblastic Leukemia (ALL)
05

Safety considerations

Drug resistance due to mutations in the ABL kinase domainSide effects associated with tyrosine kinase inhibitorsRelapseDevelopment of secondary mutations
06

Interacting drugs

Imatinib mesylate

3 more in the full profile.

07

Biomarkers

BCR-ABL transcript levelsp210 BCR-ABLp190 BCR-ABLp230 BCR-ABLb3a2 BCR-ABLb2a2 BCR-ABLe1a2 BCR-ABLe19a2 BCR-ABL

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