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TargetEnzymes

Mitogen-activated protein kinase 12

Named enzymes, including the metabolising cytochromes and the monoamine oxidases.

Measurements
4
Compounds
4
Binding constants
0
Median pX
—

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

MK12_HUMANMAPK12Homo sapiens

Mitogen-activated protein kinase 12

Serine/threonine kinase which acts as an essential component of the MAP kinase signal transduction pathway. MAPK12 is one of the four p38 MAPKs which play an important role in the cascades of cellular responses evoked by extracellular stimuli such as pro-inflammatory cytokines or physical stress leading to direct activation of transcription factors such as ELK1 and ATF2. Accordingly, p38 MAPKs phosphorylate a broad range of proteins and it has been estimated that they may have approximately 200 to 300 substrates each. Some of the targets are downstream kinases such as MAPKAPK2, which are activated through phosphorylation and further phosphorylate additional targets. Plays a role in myoblast differentiation and also in the down-regulation of cyclin D1 in response to hypoxia in adrenal cells suggesting MAPK12 may inhibit cell proliferation while promoting differentiation. Phosphorylates DLG1. Following osmotic shock, MAPK12 in the cell nucleus increases its association with nuclear DLG1, thereby causing dissociation of DLG1-SFPQ complexes. This function is independent of its catalytic activity and could affect mRNA processing and/or gene transcription to aid cell adaptation to osmolarity changes in the environment. Regulates UV-induced checkpoint signaling and repair of UV-induced DNA damage and G2 arrest after gamma-radiation exposure. MAPK12 is involved in the regulation of SLC2A1 expression and basal glucose uptake in L6 myotubes; and negatively regulates SLC2A4 expression and contraction-mediated glucose uptake in adult skeletal muscle. C-Jun (JUN) phosphorylation is stimulated by MAPK14 and inhibited by MAPK12, leading to a distinct AP-1 regulation. MAPK12 is required for the normal kinetochore localization of PLK1, prevents chromosomal instability and supports mitotic cell viability. MAPK12-signaling is also positively regulating the expansion of transient amplifying myogenic precursor cells during muscle growth and regeneration

Quoted from UniProt’s FUNCTION annotation for P53778 (reviewed).

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
DLG10.9820.6120.9000.581
MAP2K60.9800.6660.9000.386
MAPKAPK20.9740.5810.9000.364
DUSP10.9720.5260.9000.462
JUN0.9710.0900.9000.707
PTPN30.9700.5630.9000.385
MAP2K30.9690.5120.9000.319
MAPKAPK30.9670.5120.9000.306
MAPKAPK50.9660.3680.9000.503
HSPB20.9600.0910.9000.584

Where it sits in the cell

  • Nuclear speckles
  • Cytosoladditional

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Cytoplasm · Nucleus · Mitochondrion

Expression by cell type

Single cell type RNA, the 10 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Epididymal principal cells33.5 nCPM
  • Astrocytes31.8 nCPM
  • Thymic myoid cells27.2 nCPM
  • Gonadotrophs26.2 nCPM
  • Myonuclei25.4 nCPM
  • Vascular endothelial cells19.4 nCPM
  • Megakaryocytes18.5 nCPM
  • Corticotrophs17.3 nCPM
  • Megakaryocyte progenitors17.3 nCPM
  • Bergmann glia16.3 nCPM

Expression by tissue

The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.

  • skeletal muscle280.4 nTPM
  • tongue112.9 nTPM

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Other measurements 4

Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.

TargetClassTypeValue (nM)pXOrganismAssay
Mitogen-activated protein kinase 12EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1062773
Mitogen-activated protein kinase 12EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1062773
Mitogen-activated protein kinase 12EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1062773
Mitogen-activated protein kinase 12EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1062773