Tchem PKN1 Serine/threonine-protein kinase N1

Protein Summary

Description

PKC-related serine/threonine-protein kinase involved in various processes such as regulation of the intermediate filaments of the actin cytoskeleton, cell migration, tumor cell invasion and transcription regulation. Part of a signaling cascade that begins with the activation of the adrenergic receptor ADRA1B and leads to the activation of MAPK14. Regulates the cytoskeletal network by phosphorylating proteins such as VIM and neurofilament proteins NEFH, NEFL and NEFM, leading to inhibit their polymerization. Phosphorylates 'Ser-575', 'Ser-637' and 'Ser-669' of MAPT/Tau, lowering its ability to bind to microtubules, resulting in disruption of tubulin assembly. Acts as a key coactivator of androgen receptor (ANDR)-dependent transcription, by being recruited to ANDR target genes and specifically mediating phosphorylation of 'Thr-11' of histone H3 (H3T11ph), a specific tag for epigenetic transcriptional activation that promotes demethylation of histone H3 'Lys-9' (H3K9me) by KDM4C/JMJD2C. Phosphorylates HDAC5, HDAC7 and HDAC9, leading to impair their import in the nucleus. Phosphorylates 'Thr-38' of PPP1R14A, 'Ser-159', 'Ser-163' and 'Ser-170' of MARCKS, and GFAP. Able to phosphorylate RPS6 in vitro. The protein encoded by this gene belongs to the protein kinase C superfamily. This kinase is activated by Rho family of small G proteins and may mediate the Rho-dependent signaling pathway. This kinase can be activated by phospholipids and by limited proteolysis. The 3-phosphoinositide dependent protein kinase-1 (PDPK1/PDK1) is reported to phosphorylate this kinase, which may mediate insulin signals to the actin cytoskeleton. The proteolytic activation of this kinase by caspase-3 or related proteases during apoptosis suggests its role in signal transduction related to apoptosis. Alternatively spliced transcript variants encoding distinct isoforms have been observed. [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• Q16512
• A8K7W5
• B2R9R4
• B3KVN3
• Q15143
• Q504U4
• Q8IUV5
• Q9UD44

Gene Name

• PKN1

Ensembl ID

• ENST00000242783
• ENSP00000242783
• ENSG00000123143
• ENST00000342216
• ENSP00000343325

Symbol

• PAK1
• PKN
• PRK1
• PRKCL1
• DBK
• PKN
• PAK1
• PRK1
• PAK-1
• PRKCL1
• PKN-ALPHA

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
molecular function	1
drug perturbation	0.99
protein domain	0.99
biological process	0.91
hub protein	0.9

Protein Classes

PANTHER Classes

Protein / Transferase / Kinase / Protein Kinase / Non-receptor Serine/threonine Protein Kinase / Serine/threonine-protein Kinase N1

Protein / Transfer/carrier Protein / Serine/threonine-protein Kinase N1

Protein / Calcium-binding Protein / Intracellular Calcium-sensing Protein / Calmodulin / Serine/threonine-protein Kinase N1

Protein / Calcium-binding Protein / Annexin / Serine/threonine-protein Kinase N1

DTO Classes

Protein / Kinase / Protein Kinase / Agc Group / Pkn Family / Serine/threonine-protein Kinase N1

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: 190.61   (req: < 5)

Gene RIFs: 32   (req: <= 3)

Antibodies: 222   (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: 190.61   (req: >= 5)

Gene RIFs: 32   (req: > 3)

Antibodies: 222   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 31

Tchem

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

Active Ligands: 11

Tclin

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

Active Drugs: 2