Tchem CLK2 Dual specificity protein kinase CLK2

Protein Summary

Description

Dual specificity kinase acting on both serine/threonine and tyrosine-containing substrates. Phosphorylates serine- and arginine-rich (SR) proteins of the spliceosomal complex. May be a constituent of a network of regulatory mechanisms that enable SR proteins to control RNA splicing and can cause redistribution of SR proteins from speckles to a diffuse nucleoplasmic distribution. Acts as a suppressor of hepatic gluconeogenesis and glucose output by repressing PPARGC1A transcriptional activity on gluconeogenic genes via its phosphorylation. Phosphorylates PPP2R5B thereby stimulating the assembly of PP2A phosphatase with the PPP2R5B-AKT1 complex leading to dephosphorylation of AKT1. Phosphorylates: PTPN1, SRSF1 and SRSF3. Regulates the alternative splicing of tissue factor (F3) pre-mRNA in endothelial cells. This gene encodes a dual specificity protein kinase that phosphorylates serine/threonine and tyrosine-containing substrates. Activity of this protein regulates serine- and arginine-rich (SR) proteins of the spliceosomal complex, thereby influencing alternative transcript splicing. Chromosomal translocations have been characterized between this locus and the PAFAH1B3 (platelet-activating factor acetylhydrolase 1b, catalytic subunit 3 (29kDa)) gene on chromosome 19, resulting in the production of a fusion protein. Note that this gene is distinct from the TELO2 gene (GeneID:9894), which shares the CLK2 alias, but encodes a protein that is involved in telomere length regulation. There is a pseudogene for this gene on chromosome 7. Alternative splicing results in multiple transcript variants. [provided by RefSeq, Jun 2014]

Uniprot Accession IDs

• P49760
• B1AVS9
• B5MBX6
• Q96CQ0

Gene Name

• CLK2

Ensembl ID

• ENST00000361168
• ENSP00000354856
• ENSG00000176444
• ENST00000368361
• ENSP00000357345
• ENST00000572269
• ENSP00000459461
• ENSG00000261893
• ENST00000574445
• ENSP00000460443

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
small molecule	1
disease perturbation	0.95
molecular function	0.94
kinase perturbation	0.93
drug perturbation	0.87

Protein Classes

DTO Classes

Protein / Kinase / Protein Kinase / Cmgc Group / Clk Family / Dual Specificity Protein Kinase Clk2

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: 9.62   (req: < 5)

Gene RIFs: 9   (req: <= 3)

Antibodies: 300   (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: 9.62   (req: >= 5)

Gene RIFs: 9   (req: > 3)

Antibodies: 300   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 11

Tchem

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

Active Ligands: 690

Tclin

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

Active Drug: 1