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A mitogen-activated protein kinase (MAPK or MAP kinase) is a type of serine/threonine-specific protein kinases involved in directing cellular responses to a diverse array of stimuli, such as mitogens, osmotic stress, heat shock and proinflammatory cytokines.
Losmapimod (GW856553X) is an investigational drug that reached stage III clinical trials for multiple medical conditions, but did not prove efficacy. It was most recently in development by Fulcrum Therapeutics for the treatment of facioscapulohumeral muscular dystrophy (FSHD).
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.
Mitogen-activated protein kinase kinase (also known as MAP2K, MEK, MAPKK) is a dual-specificity kinase enzyme which phosphorylates mitogen-activated protein kinase (MAPK). MAP2K is classified as EC 2.7.12.2. There are seven genes: MAP2K1 (a.k.a. MEK1) MAP2K2 (a.k.a. MEK2) MAP2K3 (a.k.a. MKK3) MAP2K4 (a.k.a. MKK4) MAP2K5 (a.k.a. MKK5) MAP2K6 (a ...
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.
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.)
Encorafenib is indicated in combination with binimetinib, for the treatment of people with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test; [2] in combination with cetuximab, for the treatment of adults with metastatic colorectal cancer with a BRAF V600E mutation, as detected by an FDA-approved test, after prior therapy; [2] in ...
Oxidative stress is the most powerfully specific stress activating p38 MAPK. [7] Abnormal activity (higher or lower than physiological) of p38 has been implicated in pathological stresses in several tissues, that include neuronal, [8] [9] [10] bone, [11] lung, [12] cardiac and skeletal muscle, [13] [14] red blood cells, [15] and fetal tissues. [16]
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