MAPK Signaling - Acute Myeloid Leukemia - Melanoma - Renal Cancer - Colorectal Cancer
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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- A8716 LY3009120Target: RafSummary: Pan-RAF和RAF二聚体抑制剂
- B1135 GDC-0623Target: MEKSummary: MEK1抑制剂
- B1174 LGX818中文名: 康奈非尼Target: RafSummary: RAF抑制剂
- B1621 TAK-733Target: MEKSummary: MEK变构位点抑制剂
- A8374 AZD8330Target: MEKSummary: MEK 1/2抑制剂
- A1947 MEK162 (ARRY-162, ARRY-438162)中文名: 贝美替尼Target: MEKSummary: MEK1/2抑制剂
- A5801 BIX 02189Target: MEK|ERKSummary: MEK5抑制剂
- A5573 Pimasertib (AS-703026)Target: MEKSummary: MEK1/2抑制剂
- A5566 LY22288201 CitationTarget: p38Summary: p38 MAP激酶抑制剂
- A1632 SB202190 (FHPI)5 CitationTarget: p38Summary: P38 MAPK抑制剂