Tchem PAK3 Serine/threonine-protein kinase PAK 3

Protein Summary

Description

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. The protein encoded by this gene is a serine-threonine kinase and forms an activated complex with GTP-bound RAS-like (P21), CDC2 and RAC1. This protein may be necessary for dendritic development and for the rapid cytoskeletal reorganization in dendritic spines associated with synaptic plasticity. Defects in this gene are the cause of a non-syndromic form of X-linked intellectual disability. Alternatively spliced transcript variants encoding different isoforms have been identified. [provided by RefSeq, Jul 2017]

Uniprot Accession IDs

• O75914
• A8K389
• B1GX77
• B1GX78
• B1GX79
• Q5JWX1
• Q5JWX2
• Q7Z2D6
• Q7Z2E4
• Q7Z3Z8
• Q8WWK5
• Q8WX23
• Q9P0J8

Gene Name

• PAK3

Ensembl ID

• ENST00000262836
• ENSP00000262836
• ENSG00000077264
• ENST00000360648
• ENSP00000353864
• ENST00000372007
• ENSP00000361077
• ENST00000372010
• ENSP00000361080
• ENST00000417227
• ENSP00000389172
• ENST00000425146
• ENSP00000401982
• ENST00000446737
• ENSP00000410853
• ENST00000518291
• ENSP00000428921
• ENST00000519681
• ENSP00000429113

Symbol

• OPHN3
• ARA
• bPAK
• MRX30
• MRX47
• OPHN3
• PAK-3
• PAK3beta
• beta-PAK

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
molecular function	1
biological process	0.99
protein domain	0.85
gene perturbation	0.77
transcription factor	0.72

Protein Classes

DTO Classes

Protein / Kinase / Protein Kinase / Ste Group / Ste20 Family / Paka Subfamily / Serine/threonine-protein Kinase Pak 3

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 33.56   (req: < 5)

Gene RIFs: 27   (req: <= 3)

Antibodies: 463   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 33.56   (req: >= 5)

Gene RIFs: 27   (req: > 3)

Antibodies: 463   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 25

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 7

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 1