Molecular Target Synopsis
Domains and Structures
Drugs and Clinical Candidates
Ligand Efficiency Plot
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
Germline Genetics

PAK6 (Q9NQU5) - Overview - Molecular Target Synopsis


PAK6, Serine/threonine-protein kinase PAK 6
Enzyme Classification
UniProt Q9NQU5

Also Known as PAK6_HUMAN, PAK6, PAK5

Serine/threonine protein kinase that plays a role in the regulation of gene transcription. The kinase activity is induced by various effectors including AR or MAP2K6/MAPKK6. Phosphorylates the DNA-binding domain of androgen receptor/AR and thereby inhibits AR-mediated transcription. Inhibits also ESR1-mediated transcription. May play a role in cytoskeleton regulation by interacting with IQGAP1. May protect cells from apoptosis through phosphorylation of BAD. Interacts tightly with GTP-bound but not GDP-bound CDC42/p21 and RAC1 (By similarity). Interacts with the androgen receptor AR and the estrogen receptor ESR1. Interacts with IQGAP1 and PPM1B.

Inspect Structure
See all 3D Structures for PAK6

Isoforms / Transcripts (Protein Coding)

Sub-cellular localization

UniProt: PAK6 is active in the following subcellular-locations: cytoplasm, nucleus.
GO terms: PAK6 is active in the following subcellular-locations: cell junction, cytoplasm, fibrillar center, nucleus.

GO terms

Gene Copy Number Variation

In COSMIC - Cell Lines Project PAK6 has gain in 0 cell-lines, loss in 2 cell-lines and no signal in 1003 cell-lines. (see details)

Gene Expression

In NCI60, the highest expressing cell lines are: HCT_15, HCT_116, HCC_2998

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hs 746T, Hs 746T, NCI-H209

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, SK-N-SH, NHLF

(see details)

RNA Interference

PAK6 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: PCI30, OVTOKO. (see details)

3D Structures

For PAK6 there are:
4 structures (4 chains) solved
2 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

PAK6 is solved in complex with the approved drug(s):


(see details)
Molecular Target 3D Synopsis

Screening and Chemistry

PAK6 has been screened with 851 compounds (1580 bioactivities), 7 compounds have bioactivities that show binding affinity of <= 500nM (11 bioactivities). (see details)