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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low] HBECs were treated with a P13K inhibitor (wortman-nin), an Akt inhibitor, or an MEK1 inhibitor (U0126) chat blocks Erkl/2 activation.
The National Comprehensive Cancer Network([R]) (NCCN([R])) Oncology Research Program (ORP) has been awarded $4 million in the form of two research grants from GlaxoSmithKline (GSK) to develop studies to scientifically evaluate and define GSK2118436, a BRAF inhibitor, and GSK1120212, a MEK1 and MEK2 inhibitor.
Since it has been described that stress signaling kinases like p38 MAPK and MEK1 /2 regulate the phosphorylation, localization, and transcription of the nuclear receptor AR (Gioeli et al.
Interestingly, MEK1 /2, a central member of the MEK/ERK pathway which is activated in a range of cancer entities was shown to be slightly up-regulated on the protein level and substantially hyperphosphorylated, suggesting its activation.
These genes include protein kinases (AKT, MEK1, PIM3), growth factors (VEGF, PLGF), GTPases (RHOC, RAB11A, DEXRAS1), cytokine signaling proteins (MCP1, SOCS1, SOCS3, WSB1, IL17R), and a Wnt signaling factor (WNT4).
RAF phosphorylates and activates both MEK1 and MEK2 on two distinct serine residues (Crews et al.
However, the level of phosphorylation of MEK1 and MEK1/2 did not change, so triptolide might affect ERK1/2 activation directly.
EDT Abstract Title: "RDEA119, a Potent and Highly Selective MEK1 / 2 Inhibitor is Beneficial in Dextran Sulfate Sodium (DSS)-Induced Chronic Colitis in Mice" Poster Number: P1050 Session Title: Inflammatory Bowel Disease Location: Florida Exhibit Halls About Ardea Biosciences, Inc.
In vitro analyses indicate that XL518 is a potent and selective non-ATP-competitive inhibitor of MEK1.