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 65
Inhibitors selumetinib; U0126; N-[(2S)-2,3-dihydroxypropyl]-3-(2-fluoro-4-iodoanilino)-4-pyridinecarboxamide; 2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide; 2-(2-amino-3-methoxyphenyl)chromen-4-one; trametinib; PD318088; U0126.EtOH
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
+ down-regulates img/direct_inhibition.png phosphorylation TAL1 0.2
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation MAP2K1 0.774
Publications: 4 Organism: Mus Musculus, In Vitro
+ up-regulates img/direct-activation.png phosphorylation MAP2K1 0.551
Publications: 4 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation MAP2K1 0.641
Publications: 2 Organism: Mus Musculus
+ up-regulates activity img/direct-activation.png phosphorylation MAP2K1 0.2
Publications: 2 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation MAP2K1 0.733
Publications: 2 Organism: Homo Sapiens
Tissue: Ovary
+ up-regulates img/direct-activation.png phosphorylation MAP2K1 0.724
Publications: 2 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation MAP2K1 0.462
Publications: 1 Organism: Mus Musculus
+ up-regulates activity img/direct-activation.png phosphorylation MAP2K1 0.275
Publications: 1 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 0.559
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 0.364
Publications: 1 Organism: Homo Sapiens
Tissue: Muscle
+ down-regulates activity img/direct_inhibition.png phosphorylation CASP9 0.454
Publications: 1
+ up-regulates activity img/direct-activation.png phosphorylation MAPK1 0.735
Publications: 4 Organism: Homo Sapiens, Mus Musculus
+ up-regulates img/direct-activation.png phosphorylation MAPK3 0.737
Publications: 3 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png phosphorylation MAP2K1 0.474
Publications: 1 Organism: Mus Musculus
+ down-regulates img/direct_inhibition.png phosphorylation MAP2K1 0.469
Publications: 2 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png phosphorylation MAP2K1 0.2
Publications: 2 Organism: Chlorocebus Aethiops, Homo Sapiens
+ down-regulates activity img/direct_inhibition.png phosphorylation MAP2K1 0.735
Publications: 2 Organism: Chlorocebus Aethiops, Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation ARRB2 0.565
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation GSK3B 0.351
Publications: 1 Organism: Homo Sapiens
Tissue: Skin
+ up-regulates activity img/direct-activation.png phosphorylation MAPK3 0.737
Publications: 1 Organism: Mus Musculus
+ up-regulates img/indirect-activation.png MAP2K1 0.317
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 dephosphorylation MAP2K1 0.537
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
+ 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 0.737
Publications: 2 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
+ down-regulates activity img/direct_inhibition.png chemical inhibition MAP2K1 0.8
Publications: 1 Organism: In Vitro
+ down-regulates img/indirect_inhibition.png MAPK14 0.655
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 binding MAP2K1 0.406
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation MAP2K1 0.426
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png chemical inhibition MAP2K1 0.8
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
+ up-regulates img/direct-activation.png binding MAP2K1 0.499
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/indirect-activation.png MAP2K1 0.309
Publications: 1 Organism: Mus Musculus
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation CEBPA 0.268
Publications: 1 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 binding MAP2K1 0.596
Publications: 1 Organism: Homo Sapiens