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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B6014 BI-847325Summary: dual inhibitor of MEK and Aurora kinases -
B6024 DEL-22379Summary: inhibitor of the dimerization of ERK -
A5071 GDC-08791 CitationTarget: RafSummary: B-Raf inhibitor,potent and selective -
A1894 SL-3271 CitationTarget: MEKSummary: Selective MEK1/2 inhibitor -
A1792 PD184352 (CI-1040)Target: MEKSummary: Selective MEK inhibitor -
A1337 U0126-EtOH10 CitationTarget: MEKSummary: MEK1/2 inhibitor -
A5566 LY22288201 CitationTarget: p38Summary: P38 MAP kinase inhibitor -
A5573 Pimasertib (AS-703026)Target: MEKSummary: MEK1/2 inhibitor -
A5639 BIRB 796 (Doramapimod)1 CitationSummary: P38 MAPK inhibitor,cell permeable and highly selective -
A5707 PD318088Target: MEKSummary: Allosteric MEK1/2 inhibitor, non-ATP competitive

