Target intelligence / Profile preview

Tyrosine-protein kinase ABL2 (ABL2)

Target
ABL2
Molecular classification
Enzyme, Tyrosine Kinase, Non-receptor tyrosine kinase
01

Overview

Tyrosine-protein kinase ABL2, also known as Abelson-related gene (Arg), is a non-receptor tyrosine kinase encoded by the human ABL2 gene. It is closely related to, but distinct from, the well-known oncogene product ABL1. Both proteins share similar domain structures and overlapping cellular functions. ABL2 plays key roles in regulation of cell growth, survival, morphogenesis, motility and actin cytoskeletal structure. Deregulation or chromosomal translocations involving ABL2 are implicated in various neoplastic diseases. ABL-family kinases are targets for small molecule inhibitors like imatinib or dasatinib used clinically for chronic myeloid leukemia; these drugs inhibit both ABL1 and ARG/ABL2 kinases due to their structural similarity.

Other names
ArgAbelson-related gene
02

Mechanism of action

ATP-mimetic type I inhibitors that bind the active site of the enzyme, stabilizing a DFG-in conformation.

03

Biological functions

Regulation of cell growthRegulation of cell survivalRegulation of cell morphogenesisRegulation of cell motilityActin cytoskeletal structure regulationCytoskeletal remodelingSignal transduction
04

Disease associations

CancerLeukemiaT-cell acute lymphoblastic leukemia (T-ALL)Acute myeloid leukemia (AML)KRAS mutant non-small cell lung cancer
05

Safety considerations

Potential for off-target effects due to structural similarity with ABL1Resistance to inhibitors can develop
06

Interacting drugs

Dasatinib

1 more in the full profile.

07

Biomarkers

ABL2 expression levels in KRAS mutant non-small cell lung cancerETV6-ARG fusion in T-ALL and AML

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