MAPK Signaling
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.
- B6159 Vacquinol-1Summary: MAPK激酶4(MKK4)激活剂
- B6024 DEL-22379Summary: ERK二聚化的抑制剂
- B6014 BI-847325Summary: 丝裂原活化蛋白激酶激酶(MEK)和Aurora激酶的双重抑制剂
- B6012 Pexmetinib (ARRY-614)Target: p38|Tie-2Summary: p38 MAPK 和 Tie2/Tek 受体酪氨酸激酶的双重抑制剂
- B5960 PF-03394197(Oclacitinib)Summary: Janus激酶抑制剂
- B5942 AS601245Summary: c-Jun氨基末端蛋白激酶抑制剂
- B5866 SCH772984 HClSummary: ERK1/2抑制剂
- B5867 SCH772984 TFASummary: ERK1/2抑制剂
- A8716 LY3009120Target: RafSummary: Pan-RAF和RAF二聚体抑制剂
- B5820 RO5126766(CH5126766)Summary: Raf/MEK双重抑制剂