Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

ABL2 (P42684) - Overview - Molecular Target Synopsis

Protein


ABL2, Tyrosine-protein kinase ABL2
Enzyme Classification 2.7.10.2
UniProt P42684

Also Known as ABL2_HUMAN, ABL2, ABLL, ARG

Non-receptor tyrosine-protein kinase that plays an ABL1-overlapping role in key processes linked to cell growth and survival such as cytoskeleton remodeling in response to extracellular stimuli, cell motility and adhesion and receptor endocytosis. Coordinates actin remodeling through tyrosine phosphorylation of proteins controlling cytoskeleton dynamics like MYH10 (involved in movement); CTTN (involved in signaling); or TUBA1 and TUBB (microtubule subunits). Binds directly F-actin and regulates actin cytoskeletal structure through its F-actin-bundling activity. Involved in the regulation of cell adhesion and motility through phosphorylation of key regulators of these processes such as CRK, CRKL, DOK1 or ARHGAP35. Adhesion-dependent phosphorylation of ARHGAP35 promotes its association with RASA1, resulting in recruitment of ARHGAP35 to the cell periphery where it inhibits RHO. Phosphorylates multiple receptor tyrosine kinases like PDGFRB and other substrates which are involved in endocytosis regulation such as RIN1. In brain, may regulate neurotransmission by phosphorylating proteins at the synapse. ABL2 acts also as a regulator of multiple pathological signaling cascades during infection. Pathogens can highjack ABL2 kinase signaling to reorganize the host actin cytoskeleton for multiple purposes, like facilitating intracellular movement and host cell exit. Finally, functions as its own regulator through autocatalytic activity as well as through phosphorylation of its inhibitor, ABI1. Interacts with PSMA7. Interacts with CTTN. Found in a complex with ABL1, ABL2, CRK and UNC119; leading to the inhibition of CRK phosphorylation by ABL kinases.

5NP5
ABL2 SH3 PTYR116/161
RCSB/PDB
Inspect Structure
See all 3D Structures for ABL2

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: ABL2 is active in the following subcellular-locations: cytoplasm, cytoskeleton.
GO terms: ABL2 is active in the following subcellular-locations: actin cytoskeleton, cytosol.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project ABL2 has gain in 0 cell-lines, loss in 3 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SN12C, CAKI_1, NCI_ADR_RES

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hs 746T, HCC2885, NCI-H226

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: HSMM, NHLF, SK-N-SH

(see details)

RNA Interference


ABL2 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: SUM44, 93VU. (see details)

3D Structures


For ABL2 there are:
9 structures (15 chains) solved
3 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

ABL2 is solved in complex with the approved drug(s):

STI/IMATINIB (3GVU_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


ABL2 has been screened with 962 compounds (1675 bioactivities), 134 compounds have bioactivities that show binding affinity of <= 500nM (167 bioactivities). (see details)