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

GAK (O14976) - Overview - Molecular Target Synopsis

Protein


GAK, Cyclin-G-associated kinase
Enzyme Classification 2.7.11.1
UniProt O14976

Also Known as GAK_HUMAN, GAK

Associates with cyclin G and CDK5. Seems to act as an auxilin homolog that is involved in the uncoating of clathrin-coated vesicles by Hsc70 in non-neuronal cells. Expression oscillates slightly during the cell cycle, peaking at G1.

5Y7Z
COMPLEX STRUCTURE OF CYCLIN G-ASSOCIATED KINASE WITH GEFITINIB
RCSB/PDB
Inspect Structure
See all 3D Structures for GAK

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: GAK is active in the following subcellular-locations: cell junction, cytoplasm, focal adhesion, golgi apparatus, perinuclear region, trans-golgi network.
GO terms: GAK is active in the following subcellular-locations: cytoplasm, cytosol, focal adhesion, Golgi apparatus, intracellular membrane-bounded organelle, membrane, perinuclear region of cytoplasm, presynapse, vesicle.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project GAK has gain in 0 cell-lines, loss in 8 cell-lines and no signal in 997 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: KM12, M14, SW_620

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H520, NCI-H2009, DMS 53

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, K562, HUVEC

(see details)

RNA Interference


GAK was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: SCC90, H2342. (see details)

3D Structures


For GAK there are:
7 structures (11 chains) solved
6 are solved in complex with at least one small molecule ligand
2 are solved with an approved drug

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

IRE/GEFITINIB (5Y7Z_A, 5Y7Z_B, 5Y80_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GAK has been screened with 250 compounds (388 bioactivities), 64 compounds have bioactivities that show binding affinity of <= 500nM (96 bioactivities). (see details)