Tyrosine Kinase - EGFR - KDR - Lyn kinase - Cell Experiments
Receptor tyrosine kinases bind to extracellular ligands/growth factors, which promotes receptor dimerization and autophosphorylation of receptor tyrosine residues. This triggers a cascade of downstream events through phosphorylation of intracellular proteins that ultimately transduce the extracellular signal to the nucleus, causing changes in gene expression. Receptor tyrosine kinases include EGFR/ErbB, PDGFR, VEGFR, FGFR and MET subfamilies etc. Dysfunctions in tyrosine phosphorylation are linked to oncogenic transformation. In additions, various adaptor and effector proteins couple to carboxy-terminal of an active kinase. For instance, binding of the GRB2 adaptor protein activates EGFR and MAPK/ERK signaling.
Non-receptor tyrosine kinases involve many well-defined proteins (e.g. the Src family kinases, c-Abl, and Jak kinases) and other kinases which regulates cell growth and differentiation. For example, Src family kinases are curial for activating and inhibitory pathways in the innate immune response.
- B5648 MLR 1023Target: Lyn kinaseSummary: Lyn激酶的变构激活剂
- B1104 AZD-92911 Citation中文名: 奥希替尼Target: EGFRSummary: 突变型EGFR抑制剂。
- B1404 DCC-2036 (Rebastinib)Target: FLT3|Bcr-Abl|Tie-2|KDRSummary: Bcr-Abl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
- A8322 Neratinib (HKI-272)1 Citation中文名: 来那替尼Target: EGFRSummary: HER2/EGFR抑制剂
- A2689 Butein中文名: 紫铆因,紫铆查尔酮Target: Src|STAT|EGFR|Angiotensin-Converting Enzymes (ACEs)|5-Lipoxygenases|PTK|enoyl-acyl-carrier protein reductaseSummary: 蛋白激酶抑制剂
- A2024 PD168393Target: PDGFR|FGFR|EGFR|PKC|insulinSummary: EGFR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
- A8215 PP 1Target: Src|EGFR|JAK|ZAP-70Summary: Src家族酪氨酸激酶抑制剂
- A8219 Gefitinib (ZD1839)3 Citation中文名: 吉非替尼Target: EGFRSummary: EGFR抑制剂