Tclin GSK3A Glycogen synthase kinase-3 alpha

Protein Summary

Description

Constitutively active protein kinase that acts as a negative regulator in the hormonal control of glucose homeostasis, Wnt signaling and regulation of transcription factors and microtubules, by phosphorylating and inactivating glycogen synthase (GYS1 or GYS2), CTNNB1/beta-catenin, APC and AXIN1. Requires primed phosphorylation of the majority of its substrates. Contributes to insulin regulation of glycogen synthesis by phosphorylating and inhibiting GYS1 activity and hence glycogen synthesis. Regulates glycogen metabolism in liver, but not in muscle. May also mediate the development of insulin resistance by regulating activation of transcription factors. In Wnt signaling, regulates the level and transcriptional activity of nuclear CTNNB1/beta-catenin. Facilitates amyloid precursor protein (APP) processing and the generation of APP-derived amyloid plaques found in Alzheimer disease. May be involved in the regulation of replication in pancreatic beta-cells. Is necessary for the establishment of neuronal polarity and axon outgrowth. Through phosphorylation of the anti-apoptotic protein MCL1, may control cell apoptosis in response to growth factors deprivation. This gene encodes a multifunctional Ser/Thr protein kinase that is implicated in the control of several regulatory proteins including glycogen synthase, and transcription factors, such as JUN. It also plays a role in the WNT and PI3K signaling pathways, as well as regulates the production of beta-amyloid peptides associated with Alzheimer's disease. [provided by RefSeq, Oct 2011]

Uniprot Accession IDs

• P49840
• O14959
• GSK-3 alpha

Gene Name

• GSK3A

Ensembl ID

• ENST00000222330
• ENSP00000222330
• ENSG00000105723
• ENST00000453535
• ENSP00000412663

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
biological process	1
drug perturbation	1
kinase	0.99
molecular function	0.97
transcription factor binding site profile	0.91

Protein Classes

PANTHER Classes

Protein / Transferase / Kinase / Protein Kinase / Non-receptor Serine/threonine Protein Kinase / Glycogen Synthase Kinase-3 Alpha

DTO Classes

Protein / Kinase / Protein Kinase / Cmgc Group / Gsk Family / Gsk Subfamily / Glycogen Synthase Kinase-3 Alpha

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: 94.79   (req: < 5)

Gene RIFs: 104   (req: <= 3)

Antibodies: 1048   (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: 94.79   (req: >= 5)

Gene RIFs: 104   (req: > 3)

Antibodies: 1048   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 43

Tchem

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

Active Ligands: 162

Tclin

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

Active Drugs: 3