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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B4620 Losmapimod1 CitationSummary: p38 MAPK inhibitor, orally active -
B4727 B-Raf IN 1Summary: B-Raf inhibitor -
B4886 DTP3 TFASummary: inhibitor of GADD45β/MKK7 complex -
B4937 SB 706504Summary: p38 MAPK inhibitor -
B5126 10Z-HymenialdisineSummary: Pan kinase inhibitor -
B5130 JIP-1 (153-163)Summary: Peptide inhibitor of c-Jun N-terminal kinase (JNK) -
B5496 AMG 548Summary: P38α inhibitor,potent and selective -
B5549 PF-3644022Target: MK2Summary: Potent and Selective MK2 inhibitor -
B5593 PluripotinSummary: dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP -
B5640 HI TOPK 032Summary: T-LAK-cell-originated protein kinase (TOPK) inhibitor

