JAK/STAT Signaling - JAK
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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- B1130 GLPG06341 Citation中文名: 菲戈替尼Target: JAKSummary: JAK1抑制剂
- A4512 Cucurbitacin I中文名: 葫芦素 ITarget: STAT|JAKSummary: STAT3/JAK2信号转导抑制剂
- A4511 Cercosporamide中文名: 尾孢素酰胺Target: JAK|MNKSummary: Mnk2和JAK3抑制剂
- A3937 XL019Target: JAKSummary: 有效的JAK2选择性抑制剂
- A3741 Pyridone 6中文名: 吡啶酮6Target: JAKSummary: Pan-JAK抑制剂
- A4152 BMS-911543Target: JAKSummary: JAK2抑制剂
- A4151 ZM 39923 HClTarget: JAKSummary: 有效的JAK3选择性抑制剂
- A4150 WHI-P154Target: VEGFR|Src|EGFR|JAKSummary: JAK3抑制剂
- A4149 S-Ruxolitinib (INCB018424)中文名: 鲁索替尼Target: JAKSummary: JAK1/2抑制剂
- A4148 NVP-BSK805 2HClTarget: JAKSummary: JAK2抑制剂