Target intelligence / Profile preview

Src Family Kinases, BCR-ABL, and other Tyrosine Kinases (ABL1 (BCR-ABL for fusion protein); Src (for Src family kinases))

Target
ABL1 (BCR-ABL for fusion protein); Src (for Src family kinases)
Molecular classification
Enzyme, Kinase (specifically, tyrosine kinase), Non-receptor tyrosine kinase
01

Overview

These kinases are intracellular enzymes that transfer phosphate groups to tyrosine residues on substrate proteins, thereby modulating diverse signaling pathways regulating cell proliferation, survival, migration, and differentiation. The Src family kinases are a group of structurally related, non-receptor tyrosine kinases involved in various cell functions, whereas ABL1 is a distinct non-receptor tyrosine kinase notable for its role in cancer when aberrantly activated by fusion with BCR, forming BCR-ABL. BCR-ABL possesses constitutive kinase activity, driving oncogenesis in CML and other leukemias[1][3][6][7]. Targeted therapies, especially tyrosine kinase inhibitors (TKIs), have drastically improved patient outcomes by specifically inhibiting these kinases and their pathological signaling[2][3][5]. This composite target entry should be broken down into its specific kinase components for precise structured annotation. Each kinase (e.g., ABL1, Src, Fyn) would merit its own profile.

Other names
BCR-ABL: Breakpoint Cluster Region-Abelson fusion proteinABL1: c-Abl, Abelson tyrosine kinaseSrc family: Src, Fyn, Yes, Lck, Lyn, Hck, Blk, FgrNon-receptor tyrosine kinases
02

Mechanism of action

ATP-competitive inhibition of kinase catalytic activity - Inhibition of autophosphorylation and substrate phosphorylation - Blockade of oncogenic downstream signaling (e.g., STAT5, Crkl phosphorylation)

03

Biological functions

Signal transductionCell cycle regulationApoptosis modulationImmune response coordinationCell proliferation
04

Disease associations

Cancer (especially chronic myelogenous leukemia, acute lymphoblastic leukemia)InflammationCardiovascular disease (via modulation of vascular cell biology)Neurodegenerative disease (some Src family kinases)
05

Safety considerations

Myelosuppression (neutropenia, thrombocytopenia)Vascular occlusive events (for ponatinib)Off-target effects and resistance mutationsQT prolongation (for nilotinib)Liver toxicity
06

Interacting drugs

6 more in the full profile.

07

Biomarkers

BCR-ABL transcript detection (PCR)STAT5 phosphorylation statusCrkl phosphorylation status

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