JAK/STAT Signaling
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.
- A1845 Canertinib (CI-1033)中文名: 卡奈替尼Summary: HER家族酪氨酸激酶抑制剂
- A1393 WZ8040Target: EGFRSummary: EGFR T790M抑制剂
- A1835 Pelitinib (EKB-569)中文名: 培利替尼Summary: 有效的EGFR不可逆抑制剂
- A2412 CP-724714Target: VEGFR|PDGFR|Bcr-Abl|Src|EGFR|c-MET|Insulin Receptors|IRG-1RSummary: 有效的HER2选择性抑制剂
- A1389 WZ4002Summary: 突变型(L858R,T790M)EGFR抑制剂
- A8247 Afatinib (BIBW2992)1 Citation中文名: 阿法替尼Target: EGFRSummary: EGFR/ HER2抑制剂
- A8234 Erlotinib Hydrochloride2 Citation中文名: 盐酸厄洛替尼Summary: EGFR抑制剂
- A8219 Gefitinib (ZD1839)3 Citation中文名: 吉非替尼Target: EGFRSummary: EGFR抑制剂
- A8218 Lapatinib2 Citation中文名: 拉帕替尼Target: ErbBSummary: EGFR/HER2抑制剂
- A3967 Lapatinib Ditosylate中文名: 二苯磺酸拉帕替尼Target: EGFR|ErbB-2Summary: EGFR / HER2抑制剂