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

PAK6 (Q9NQU5) - Overview - Molecular Target Synopsis

Protein


PAK6, Serine/threonine-protein kinase PAK 6
Enzyme Classification 2.7.11.1
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.

4KS7
PAK6 KINASE DOMAIN IN COMPLEX WITH PF-3758309
RCSB/PDB
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.



UniProt
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):

B49/SUNITINIB (4KS8_A).

(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)