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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A8207 AZD6244 (Selumetinib)6 CitationSummary: MEK inhibitor -
A8254 SB 20358038 CitationTarget: p38|PKBSummary: P38 MAP kinase inhibitor -
A4746 Afatinib2 CitationSummary: A covalent inhibitor targeting members of the ErbB family -
C8553 SPOP-IN-1 -
A8226 TAK-632Target: RafSummary: Pan-RAF inhibitor,potent and selective -
A8245 Sorafenib Tosylate1 CitationTarget: Raf|VEGFRSummary: Raf kinases and tyrosine kinases inhibitor -
A4604 SP 60012531 CitationTarget: JNKSummary: JNK1/2/3 inhibitor -
A1663 PD980599 CitationTarget: MEKSummary: MEK inhibitor,selective and reversible -
A5071 GDC-08791 CitationTarget: RafSummary: B-Raf inhibitor,potent and selective -
A1894 SL-3271 CitationTarget: MEKSummary: Selective MEK1/2 inhibitor

