Tchem RPS6KA4 Ribosomal protein S6 kinase alpha-4

Protein Summary

Description

Serine/threonine-protein kinase that is required for the mitogen or stress-induced phosphorylation of the transcription factors CREB1 and ATF1 and for the regulation of the transcription factor RELA, and that contributes to gene activation by histone phosphorylation and functions in the regulation of inflammatory genes. Phosphorylates CREB1 and ATF1 in response to mitogenic or stress stimuli such as UV-C irradiation, epidermal growth factor (EGF) and anisomycin. Plays an essential role in the control of RELA transcriptional activity in response to TNF. Phosphorylates 'Ser-10' of histone H3 in response to mitogenics, stress stimuli and EGF, which results in the transcriptional activation of several immediate early genes, including proto-oncogenes c-fos/FOS and c-jun/JUN. May also phosphorylate 'Ser-28' of histone H3. Mediates the mitogen- and stress-induced phosphorylation of high mobility group protein 1 (HMGN1/HMG14). In lipopolysaccharide-stimulated primary macrophages, acts downstream of the Toll-like receptor TLR4 to limit the production of pro-inflammatory cytokines. Functions probably by inducing transcription of the MAP kinase phosphatase DUSP1 and the anti-inflammatory cytokine interleukin 10 (IL10), via CREB1 and ATF1 transcription factors. This gene encodes a member of the RSK (ribosomal S6 kinase) family of serine/threonine kinases. This kinase contains 2 non-identical kinase catalytic domains and phosphorylates various substrates, including CREB1 and ATF1. The encoded protein can also phosphorylate histone H3 to regulate certain inflammatory genes. Several transcript variants encoding different isoforms have been found for this gene. [provided by RefSeq, Jan 2016]

Uniprot Accession IDs

• O75676
• A8K7Z8
• O75585
• Q53ES8
• S6K-alpha-4

Gene Name

• RPS6KA4

Ensembl ID

• ENST00000334205
• ENSP00000333896
• ENSG00000162302

Symbol

• MSK2
• MSK2
• RSK-B
• S6K-alpha-4

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
interacting protein	1
drug perturbation	0.99
molecular function	0.99
protein domain	0.97
disease perturbation	0.93

Protein Classes

DTO Classes

Protein / Kinase / Protein Kinase / Agc Group / Rsk Family / Msk Subfamily / Ribosomal Protein S6 Kinase Alpha-4

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: 22.82   (req: < 5)

Gene RIFs: 9   (req: <= 3)

Antibodies: 240   (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: 22.82   (req: >= 5)

Gene RIFs: 9   (req: > 3)

Antibodies: 240   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 18

Tchem

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

Active Ligands: 6

Tclin

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

Active Drug: 0