MAPK/ERK


The mitogen-activated protein kinase (MAPK) is a highly conserved family of serine/threonine kinases that mediate a board range of cellular processes, including proliferation, differentiation, motility, migration, stress response, apoptosis and survival. The activation of MAPK involves signaling pathways consisting of MAPK kinase (i.e. MAPKKK or MEKK) that activates MAPK/ERK (i.e. MAPKK or MEK). A variety of extracellular signals such as mitogens, cytokines, growth factors, and environmental stressors stimulate a phosphorylation-dependent increase in the activity of MAPK.
Activated MAPKs transduce the phosphorylation and activation of MAPK-activated protein kinases (MAPKAPKs), e.g. RSK, MSK, or MNK family, and MK2/3/5. There are three main MAPK families, signal-regulated kinase 1 and 2 (Erk1/2 or p44/42), the c-Jun N-terminal kinases 1-3 (JNK1-3)/ stress activated protein kinases (SAPK1A, 1B, 1C), the p38 isoforms (p38α, β, γ, and δ). ERK signaling is involved in cell division, migration and survival. p38 MAPK and JNK/SAPK pathways are activated by cellular stress. The p38 MAPK pathway regulates cell motility, transcription, and chromatin remodeling. JNK/SAPK signaling affects apoptosis and inflammation. Dysregulation of MAPK pathway results in tumorgenesis and other pathological conditions.
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B5960 PF-03394197(Oclacitinib)Summary: Novel Janus kinase inhibitor -
B6012 Pexmetinib (ARRY-614)2 CitationTarget: p38|Tie-2Summary: dual inhibitor of p38 MAPK and Tie2/Tek receptor tyrosine kinase -
B6014 BI-847325Summary: dual inhibitor of MEK and Aurora kinases -
B6024 DEL-22379Summary: inhibitor of the dimerization of ERK -
A8724 ONC201Summary: A DRD2 antagonist and ClpP activator, and also an inhibitor of the AKT and ERK pathways. -
A8226 TAK-632Target: RafSummary: Pan-RAF inhibitor,potent and selective -
A8245 Sorafenib Tosylate1 CitationTarget: Raf|VEGFRSummary: Raf kinases and tyrosine kinases inhibitor -
A8254 SB 20358043 CitationTarget: p38|PKBSummary: P38 MAP kinase inhibitor -
A1663 PD9805925 CitationTarget: MEKSummary: MEK inhibitor,selective and reversible -
A5071 GDC-08791 CitationTarget: RafSummary: B-Raf inhibitor,potent and selective

