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

PAK3 (O75914) - Overview - Molecular Target Synopsis

Protein


PAK3, Serine/threonine-protein kinase PAK 3
Enzyme Classification 2.7.11.1
UniProt O75914

Also Known as PAK3_HUMAN, PAK3, OPHN3

Serine/threonine protein kinase that plays a role in a variety of different signaling pathways including cytoskeleton regulation, cell migration, or cell cycle regulation. Plays a role in dendrite spine morphogenesis as well as synapse formation and plasticity. Acts as downstream effector of the small GTPases CDC42 and RAC1. Activation by the binding of active CDC42 and RAC1 results in a conformational change and a subsequent autophosphorylation on several serine and/or threonine residues. Phosphorylates MAPK4 and MAPK6 and activates the downstream target MAPKAPK5, a regulator of F-actin polymerization and cell migration. Additionally, phosphorylates TNNI3/troponin I to modulate calcium sensitivity and relaxation kinetics of thin myofilaments. May also be involved in early neuronal development. Interacts tightly with GTP-bound but not GDP-bound CDC42/p21 and RAC1. Shows highly specific binding to the SH3 domains of phospholipase C-gamma and of adapter protein NCK. Interacts with the C-terminal of APP (By similarity). Interacts with ARHGEF6 and ARHGEF7.

6FD3
THIOPHOSPHORYLATED PAK3 KINASE DOMAIN
RCSB/PDB
Inspect Structure
See all 3D Structures for PAK3

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: PAK3 is active in the following subcellular-locations: cytoplasm.
GO terms: PAK3 is active in the following subcellular-locations: cytoplasm, cytosol, endosome, glutamatergic synapse, plasma membrane, postsynaptic density.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project PAK3 has gain in 0 cell-lines, loss in 32 cell-lines and no signal in 973 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: NCI_H460, UO_31, HOP_92

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H460, HCC515, DMS 79

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, NHLF, HSMM

(see details)

RNA Interference


PAK3 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: HCC1954, COV504. (see details)

3D Structures


For PAK3 there are:
1 structures (1 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


PAK3 has been screened with 698 compounds (1314 bioactivities), 16 compounds have bioactivities that show binding affinity of <= 500nM (24 bioactivities). (see details)