MAP2K1

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MAP2K1

A gene on chromosome 15q22.1-q22.33 that encodes a dual-specificity protein kinase which is an essential component of the MAP-kinase signal transduction pathway. MAP2K1 binds to extracellular ligands (e.g., as growth factors, cytokines and hormones) to their cell surface
receptors, activating RAS and RAF1, which in turn activates dual-specificity protein kinases MAP2K1/MEK1 and MAP2K2/MEK2; these act in the MAPK/ERK cascade and catalyse the phosphorylation of threonine and tyrosine residues, leading to the activation of the extracellular signal-regulated kinases MAPK3/ERK1 and MAPK1/ERK2,  and amplification of the transduction signal within the MAPK/ERK cascade.
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Phosphorylation of p38MAPK [Figure 7], P < 0.05] and MEK1 [Figure 8], P < 0.05] in HK-2 cells at 2, 6, and 12 h was increased by 75%, 130%, 215%, and 74%, 183%, 262%, respectively, as compared to that at 0 h.
(28) Activated Raf (or other MAP3K) binds and phosphorylates downstream kinase MEK1 and MEK2 with dual specificity, which in turn phosphorylate ERK1/2.
Hollingsworth, "Partner choice during meiosis is regulated by Hop1-promoted dimerization of Mek1," Molecular Biology of the Cell, vol.
NS ile iliskilendirilen 12q24.1 kromozomdaki PTPN11 (protein tirozin fosfataz, non-reseptor tip 11) genindeki yanlis anlamli mutasyonlarin yani sira RAS-MAPK (mitojen ile harekete gecmis protein kinaz) yolagi ile iliskili olan SOS1, RAF1, MEK1, KRAS gen mutasyonlari da NS'li hastalarda degisen oranlarda bildirilmistir (9-14).
Este grupo de pesquisa, mais tarde (Aronson e colaboradores, 1997), mostrou que p42 e p44MAPK (isto e, ERK1/2) foram fosforilados em amostras de musculo esqueletico de seres humanos, apos exercicio em bicicleta ergometrica, seguido de ativacao de MEK1 e Raf-1.
Incubation of RA SF with PD98059 or UO126, selective inhibitors of the MAPKK Mek1 (proximal activator of Erk), dramatically inhibited MMP-1 secretion in response to IL-1[beta] or TNF-[alpha].
For example, kinases in the MAP kinase signal transduction pathway, such as Erk1/2, are activated by MEK1 phosphorylation at residues T183 and Y185, respectively, and inactivated by dephosphorylation by ser/thr phosphatases, tyrosine-specific phosphatases, or dual-acting phosphatases (Cohen, 2000; Keyse, 2000).
By selectively inhibiting MEK1 and MEK2, U0126 signal transduction agent functionally antagonizes AP1-mediated transcriptional activation.
- The European Commission has granted Orphan Drug Designation for mirdametinib (formerly PD-0325901), an oral, small molecule inhibitor of MEK1 and MEK2, for the treatment of neurofibromatosis type 1, US-based clinical-stage biopharmaceutical company SpringWorks Therapeutics, Inc.
MEK1 and MEK2 are serine/threonine protein kinases that act downstream of RAS and RAF to activate ERK.
MAP2K1 (MEK1) mutations define a distinct subset of lung adenocarcinoma associated with smoking.
Further mechanisms of MAPK pathway acquired resistance to single agent inhibition include ERK-mediated gainof-function MEK1 mutations, BRAF amplification, and KRAS alterations [137, 138].