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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A5071 GDC-08791 CitationTarget: RafSummary: B-Raf inhibitor,potent and selective -
A1894 SL-3271 CitationTarget: MEKSummary: Selective MEK1/2 inhibitor -
B1172 B-Raf inhibitor 1Summary: Potent and selective B-Raf inhibitor -
B1173 B-Raf inhibitor 1 dihydrochlorideSummary: B-Raf inhibitor,potent and selective -
B1407 Dabrafenib (GSK2118436)3 CitationTarget: RafSummary: Inhibitor of BRAF(V600) mutants -
B1267 RefametinibTarget: MEKSummary: MEK 1/ MEK 2 inhibitor -
BA2736 TakinibSummary: Takinib (EDHS-206) is a potent and selective inhibitor (=9.5nM) -
BA2741 APTO-253Summary: APTO-253 (LOR-253) is a small molecule that inhibits expression, stabilizes G-quadruplex DNA and induces cell cycle arrest and apoptosis in AML cells. -
BA2754 RMC-6291Summary: RMC-6291 is an orally effective covalent inhibitor. -
BA2788 LysophosphatidylcholinesSummary: Lysophosphatidylcholines are orally active lysophosphatidylcholines and a component of oxidized low-density lipoprotein (LDL).

