Target intelligence / Profile preview

Breakpoint cluster region protein (BCR)

Target
BCR
Molecular classification
Enzyme, Kinase (Serine/threonine kinase), GTPase-activating protein (GAP), Guanine nucleotide exchange factor (GEF)
01

Overview

The **breakpoint cluster region protein** (BCR) is a multidomain enzyme with serine/threonine kinase activity, GTPase-activating protein (GAP) activity, and guanine nucleotide exchange factor (GEF) activity for the Rho family of GTPases, including Rac1 and RhoA[1][2][3][8]. BCR plays important roles in cellular signaling pathways that regulate cytoskeletal organization and cell migration. Clinical significance arises predominantly from chromosomal translocation t(9;22) leading to the BCR-ABL1 fusion gene, which encodes a constitutively active tyrosine kinase and is the hallmark of chronic myeloid leukemia and some acute leukemias. BCR itself participates in various signaling interactions, but it is as the BCR-ABL1 fusion oncoprotein that it is targeted therapeutically[1][2][3][8].

Other names
BCR activator of RhoGEF and GTPaserenal carcinoma antigen NY-REN-26BCR1D22S11D22S662CMLPHLALLbreakpoint cluster region protein isoform 1breakpoint cluster region protein isoform 2
02

Mechanism of action

Tyrosine kinase inhibition (by targeting the abnormal BCR-ABL1 fusion protein activity, which drives unregulated cell growth)

03

Biological functions

Signal transductionRegulation of Rho family GTPases (including Rac1 and RhoA)Cell movement (migration)Regulation of cytoskeletal organizationCell proliferation
04

Disease associations

Cancer (especially chronic myeloid leukemia, B-cell acute lymphoblastic leukemia, and rarely acute myeloid leukemia)Other cancers (implicated via BCR-ABL1 fusion)
05

Safety considerations

Therapeutic resistance (mutation in BCR-ABL1 can confer resistance to kinase inhibitors)Off-target effects of tyrosine kinase inhibitors (can affect other kinases)
06

Interacting drugs

4 more in the full profile.

07

Biomarkers

BCR-ABL1 fusion gene (Philadelphia chromosome) is used as a biomarker for diagnosis and monitoring of chronic myeloid leukemia and some acute leukemias

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