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

PAK5 (Q9P286) - Overview - Molecular Target Synopsis

Protein


PAK5, Serine/threonine-protein kinase PAK 5
Enzyme Classification 2.7.11.1
UniProt Q9P286

Also Known as PAK5_HUMAN, PAK5, KIAA1264, PAK7

Serine/threonine protein kinase that plays a role in a variety of different signaling pathways including cytoskeleton regulation, cell migration, proliferation or cell survival. Activation by various effectors including growth factor receptors or active CDC42 and RAC1 results in a conformational change and a subsequent autophosphorylation on several serine and/or threonine residues. Phosphorylates the proto-oncogene RAF1 and stimulates its kinase activity. Promotes cell survival by phosphorylating the BCL2 antagonist of cell death BAD. Phosphorylates CTNND1, probably to regulate cytoskeletal organization and cell morphology. Keeps microtubules stable through MARK2 inhibition and destabilizes the F-actin network leading to the disappearance of stress fibers and focal adhesions. Interacts tightly with GTP-bound but not GDP-bound CDC42/p21 and RAC1. Interacts with MARK2, leading to inhibit MARK2 independently of kinase activity. Interacts with RHOD and RHOH.

2F57
CRYSTAL STRUCTURE OF THE HUMAN P21-ACTIVATED KINASE 5
RCSB/PDB
Inspect Structure
See all 3D Structures for PAK5

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
719ENSG00000101349ENST00000378423, ENST00000353224, ENST00000378429ENSP00000367679, ENSP00000322957, ENSP00000367686Q9P286-1

Sub-cellular localization


UniProt: PAK5 is active in the following subcellular-locations: cytoplasm, mitochondrion, nucleus.
GO terms: PAK5 is active in the following subcellular-locations: cytoplasm, mitochondrion, nucleoplasm, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project PAK5 has gain in 3 cell-lines, loss in 2 cell-lines and no signal in 1000 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are:

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

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:

(see details)

RNA Interference


PAK5 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: HS578T, COV362. (see details)

3D Structures


For PAK5 there are:
1 structures (2 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


PAK5 has been screened with 839 compounds (1565 bioactivities), 11 compounds have bioactivities that show binding affinity of <= 500nM (15 bioactivities). (see details)