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A MEK inhibitor is a chemical or drug that inhibits the mitogen-activated protein kinase enzymes MEK1 and/or MEK2. They can be used to affect the MAPK/ERK pathway which is often overactive in some cancers. (See MAPK/ERK pathway#Clinical significance.)
To understand the dynamics of EGFR-ERK pathway, specifically how is the frequency and amplitude modulated, they applied the EGFR inhibitor gefitinib or the highly selective MAPK/ERK kinase (MEK) inhibitor PD0325901 (PD). Two inhibitors yield actually a little bit different result: gefitinib, at intermediate concentration, would induce pulsatory ...
It is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase. [10] [11] U0126 was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with IC 50 of 72 nM for MEK1 and 58 nM for MEK2.
The mating MAPK pathway consist of three tiers (Ste11-Ste7-Fus3), but the MAP2 and MAP3 kinases are shared with another pathway, the Kss1 or filamentous growth pathway. While Fus3 and Kss1 are closely related ERK-type kinases, yeast cells can still activate them separately, with the help of a scaffold protein Ste5 that is selectively recruited ...
Tyrosine kinase inhibitor (TKI) with selective activity against RET, VEGFR-2 and EGFR: Medullary thyroid cancer. Diarrhoea, hypertension, QT interval prolongation, depression, electrolyte anomalies, hypothyroidism and GI perforation (uncommon). 2.3 mTOR inhibitors: Everolimus: PO: mTOR inhibitor.
MLK, a type of MAPKKK, are associated with Parkinson's disease and inhibitors to the MLK proteins have been shown to treat Parkinson's disease. The MAPKKK pathways and specifically the over-expression of cascades of JNK and p38 are also involved in Crohn's disease and polycystic kidney disease. Inhibitors of these pathways help in treating the ...
NJK14047 is a drug which acts as a selective inhibitor of the enzyme p38 mitogen-activated protein kinase (p38 MAPK). It has antiviral and antiinflammatory effects and was originally developed as a potential treatment for inflammatory lung conditions such as influenza.
Selumetinib is a kinase inhibitor, more specifically a selective inhibitor of the enzyme mitogen-activated protein kinase kinase (MAPK kinase or MEK) subtypes 1 and 2. These enzymes are part of the MAPK/ERK pathway, which regulates cell proliferation (i.e., growth and division) and is overly active in many types of cancer. [18]