Summary

Name MAP2K1
Full Name Dual specificity mitogen-activated protein kinase kinase 1
Synonyms MAP kinase kinase 1, MAPKK 1, MKK1, ERK activator kinase 1, MAPK/ERK kinase 1, MEK 1 | MEK1, PRKMK1
Primary ID Q02750
Links - -
Type protein
Relations 74
Inhibitors N-[(2S)-2,3-dihydroxypropyl]-3-(2-fluoro-4-iodoanilino)-4-pyridinecarboxamide; 2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide; PD318088; U0126; U0126.EtOH; trametinib; selumetinib; 2-(2-amino-3-methoxyphenyl)chromen-4-one
Function Dual specificity protein kinase which acts as an essential component of the MAP kinase signal transduction pathway. Binding of extracellular ligands such as growth factors, cytokines and hormones to their cell-surface receptors activates RAS and this initiates RAF1 activation. RAF1 then further activates the dual-specificity protein kinases MAP2K1/MEK1 and MAP2K2/MEK2. Both MAP2K1/MEK1 and MAP2K2/MEK2 function specifically in the MAPK/ERK cascade, and catalyze the concomitant phosphorylation of a threonine and a tyrosine residue in a Thr-Glu-Tyr sequence located in the extracellular signal-regulated kinases MAPK3/ERK1 and MAPK1/ERK2, leading to their activation and further transduction of the signal within the MAPK/ERK cascade. Activates BRAF in a KSR1 or KSR2-dependent manner; by binding to KSR1 or KSR2 releases the inhibitory intramolecular interaction between KSR1 or KSR2 protein kinase and N-terminal domains which promotes KSR1 or KSR2-BRAF dimerization and BRAF activation (PubMed:29433126). Depending on the cellular context, this pathway mediates diverse biological functions such as cell growth, adhesion, survival and differentiation, predominantly through the regulation of transcription, metabolism and cytoskeletal rearrangements. One target of the MAPK/ERK cascade is peroxisome proliferator-activated receptor gamma (PPARG), a nuclear receptor that promotes differentiation and apoptosis. MAP2K1/MEK1 has been shown to export PPARG from the nucleus. The MAPK/ERK cascade is also involved in the regulation of endosomal dynamics, including lysosome processing and endosome cycling through the perinuclear recycling compartment (PNRC), as well as in the fragmentation of the Golgi apparatus during mitosis.

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Modifications Tables

Relations

Regulator Mechanism target score
+ up-regulates quantity by stabilization img/direct-activation.png phosphorylation TET2 0.25
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png phosphorylation TAL1 0.2
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation MAP2K1 0.738
Publications: 2 Organism: Homo Sapiens
Tissue: Ovary
+ up-regulates img/direct-activation.png phosphorylation MAP2K1 0.564
Publications: 4 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation MAP2K1 0.2
Publications: 2 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation MAP2K1 0.729
Publications: 2 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation MAP2K1 0.649
Publications: 2 Organism: Mus Musculus
+ up-regulates activity img/direct-activation.png phosphorylation MAP2K1 0.777
Publications: 4 Organism: Mus Musculus, In Vitro
+ up-regulates activity img/direct-activation.png phosphorylation MAP2K1 0.274
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation MAP2K1 0.475
Publications: 1 Organism: Mus Musculus
+ up-regulates activity img/direct-activation.png phosphorylation HSF1 0.288
Publications: 4 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation MAP2K1 0.2
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation MAP2K1 0.571
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation MAP2K1 0.2
Publications: 1 Organism: In Vitro
+ down-regulates img/direct_inhibition.png phosphorylation IRS1 0.361
Publications: 1 Organism: Homo Sapiens
Tissue: Muscle
+ up-regulates activity img/direct-activation.png phosphorylation RAF1 0.738
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png phosphorylation CASP9 0.446
Publications: 1
+ up-regulates activity img/direct-activation.png phosphorylation MAPK1 0.74
Publications: 4 Organism: Homo Sapiens, Mus Musculus
+ up-regulates img/direct-activation.png phosphorylation MAPK3 0.742
Publications: 3 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png phosphorylation MAP2K1 0.484
Publications: 2 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png phosphorylation MAP2K1 0.489
Publications: 1 Organism: Mus Musculus
+ down-regulates activity img/direct_inhibition.png phosphorylation MAP2K1 0.74
Publications: 2 Organism: Chlorocebus Aethiops, Homo Sapiens
+ down-regulates activity img/direct_inhibition.png phosphorylation MAP2K1 0.2
Publications: 2 Organism: Chlorocebus Aethiops, Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation ARRB2 0.576
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation GSK3B 0.346
Publications: 1 Organism: Homo Sapiens
Tissue: Skin
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation CEBPA 0.267
Publications: 1 Organism: Mus Musculus
+ down-regulates img/direct_inhibition.png chemical inhibition MAP2K1 0.8
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition MAP2K1 0.8
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation ERK1/2 0.742
Publications: 2 Organism: Mus Musculus
+ down-regulates img/direct_inhibition.png chemical inhibition MAP2K1 0.8
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation Gbeta 0.2
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition MAP2K1 0.8
Publications: 2 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation MAPK3 0.742
Publications: 1 Organism: Mus Musculus
+ down-regulates activity img/direct_inhibition.png phosphorylation MYT1 0.265
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png chemical inhibition MAP2K1 0.8
Publications: 1 Organism: In Vitro
+ down-regulates activity img/direct_inhibition.png phosphorylation MYRF 0.261
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition MAP2K1 0.8
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation MAP2K1 0.337
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png binding MAP2K1 0.403
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png chemical inhibition MAP2K1 0.8
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/indirect_inhibition.png MAPK14 0.662
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/indirect-activation.png MAP2K1 0.315
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding MAP2K1 0.608
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding MAP2K1 0.513
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png dephosphorylation MAP2K1 0.551
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png chemical inhibition MAP2K1 0.8
Publications: 1 Organism: In Vitro
+ down-regulates img/direct_inhibition.png chemical inhibition MAP2K1 0.8
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition MAP2K1 0.8
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition MAP2K1 0.8
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/indirect-activation.png MAP2K1 0.306
Publications: 1 Organism: Mus Musculus
+ up-regulates img/direct-activation.png phosphorylation MAP2K1 0.418
Publications: 1 Organism: Homo Sapiens