JAK/STAT Signaling - Animal Experiments
The JAK (Janus kinase) / STAT (signal transducer and activator of transcription) signaling pathway transduce signals that are essential for development, cellular differentiation and homeostasis. This pathway plays a critical role in cytokine receptor systems, regulating growth, survival and pathogen resistance. JAK is a family of non-receptor protein tyrosine kinases, consisting of JAK1, JAK2, JAK3 and TYK2 (Tyrosine Kinase-2). STATs are transcription factors that activated following recruitment to an activated receptor complex, seven STAT proteins have been identified: STAT1, STAT2, STAT3, STAT4, STAT5A, STAT5B and STAT6.
Various ligands including cytokines (e.g. interferons and interleukins), hormones (e.g. erythropoietin and growth hormone) and their cell surface receptors activate JAK proteins, which autophosphorylate, and then phosphorylate the receptor. Subsequently, JAKs phosphorylate a specific tyrosine residue on the STAT protein, promoting dimerization via SH2 domains. The activated STATs form homo-/heterodimers and translocate to the nucleus to trigger target gene transcription. In addition, suppressors of cytokine signaling (SOCS) family inhibit receptor signaling via homologous or heterologous feedback regulation. Dysregulation in JAK/STAT signaling is associated with diseases such as atherosclerosis, immunodeficiencies and cancer.
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- B5836 AZ5104Target: EGFRSummary: EGFR抑制剂
- B4970 HO-38671 CitationTarget: STATSummary: STAT3抑制剂
- B2283 Niclosamide中文名: 氯硝柳胺Target: STATSummary: STAT3信号通路抑制剂
- B1130 GLPG06341 Citation中文名: 菲戈替尼Target: JAKSummary: JAK1抑制剂
- B1104 AZD-92911 Citation中文名: 奥希替尼Target: EGFRSummary: 突变型EGFR抑制剂。
- A8375 AZD8931 (Sapitinib)中文名: 沙普替尼Target: EGFR|ErbBSummary: ErbB抑制剂
- A8366 ARRY-380Target: HER2Summary: 酪氨酸激酶HER2和P95-HER2抑制剂。
- A8357 AG-1478中文名: 酪氨酸磷酸化抑制剂 AG-1478Target: EGFRSummary: EGFR抑制剂
- A8338 NSC 748595 CitationTarget: STATSummary: Stat3抑制剂
- A8322 Neratinib (HKI-272)1 Citation中文名: 来那替尼Target: EGFRSummary: HER2/EGFR抑制剂