MAPK Signaling - Raf - GABAA Receptors - JNK - 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
- A8313 RAF265Target: Raf|VEGFRSummary: 多细胞激酶抑制剂
- A5071 GDC-08791 CitationTarget: RafSummary: B-Raf抑制剂
- A4604 SP 6001257 CitationTarget: JNKSummary: JNK1/2/3抑制剂
- A8245 Sorafenib Tosylate1 Citation中文名: 甲苯磺酸索拉非尼Target: Raf|VEGFRSummary: Raf激酶和酪氨酸激酶抑制剂
- A8226 TAK-632Target: RafSummary: Pan-RAF的强效选择性抑制剂
- A3347 Dabrafenib Mesylate (GSK-2118436)中文名: 达帕菲尼甲磺酸盐Target: RafSummary: BRAF(V600E)抑制剂
- A3016 PLX-47201 CitationTarget: RafSummary: BRAF激酶抑制剂
- A3009 Sorafenib2 Citation中文名: 索拉非尼Target: Raf|VEGFRSummary: Raf激酶和酪氨酸激酶抑制剂
- A3004 Vemurafenib (PLX4032, RG7204)9 Citation中文名: 维罗非尼Target: RafSummary: BRAF激酶抑制剂