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

ILK (Q13418) - Overview - Molecular Target Synopsis

Protein


ILK, Integrin-linked protein kinase
Enzyme Classification 2.7.11.1
UniProt Q13418

Also Known as ILK_HUMAN, ILK, ILK1, ILK2

Receptor-proximal protein kinase regulating integrin-mediated signal transduction (PubMed:8538749, PubMed:9736715). May act as a mediator of inside-out integrin signaling. Focal adhesion protein part of the complex ILK-PINCH. This complex is considered to be one of the convergence points of integrin- and growth factor-signaling pathway. Could be implicated in mediating cell architecture, adhesion to integrin substrates and anchorage-dependent growth in epithelial cells. Phosphorylates beta-1 and beta-3 integrin subunit on serine and threonine residues, but also AKT1 and GSK3B (PubMed:8538749, PubMed:9736715). Interacts with FERMT2 (By similarity). Interacts with the cytoplasmic domain of ITGB1. Could also interact with integrin ITGB2, ITGB3 and/or ITGB5. Interacts (via ANK repeats) with LIMS1 and LIMS2. Interacts with PARVA and PARVB; these compete for the same binding site. Interacts probably also with TGFB1I1. Interacts (via ANK repeats) with EPHA1 (via SAM domain); stimulated by EFNA1 but independent of the kinase activity of EPHA1. Interacts with LIMD2; leading to activate the protein kinase activity (PubMed:24590809).

6MIB
CRYSTAL STRUCTURE OF THE ILK ATP-BINDING DEFICIENT MUTANT (L207W) /ALPHA-PARVIN CORE COMPLEX
RCSB/PDB
Inspect Structure
See all 3D Structures for ILK

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: ILK is active in the following subcellular-locations: cell junction, cell membrane, cell projection, cytoplasm, focal adhesion, lamellipodium, myofibril, sarcomere.
GO terms: ILK is active in the following subcellular-locations: cell junction, cell-cell junction, costamere, cytosol, dendritic shaft, focal adhesion, lamellipodium, membrane, neuronal cell body, nucleoplasm, plasma membrane, protein-containing complex, sarcomere, stress fiber, terminal bouton.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project ILK 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: HS578T, SN12C, MDA_MB_231

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: G44, G121, G61

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: SK-N-SH, BJ, NHLF

(see details)

RNA Interference


ILK was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: TE9, JIMT1. (see details)

3D Structures


For ILK there are:
9 structures (9 chains) solved
2 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


ILK has been screened with 199 compounds (353 bioactivities), 76 compounds have bioactivities that show binding affinity of <= 500nM (151 bioactivities). (see details)