Tyrosine Kinase - DCLK2 - PKC - Src - Animal 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.
- B5839 SU6656Target: Src|Lyn|YES|FynSummary: Src 酪氨酸激酶抑制剂
- 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
- A5467 Ponatinib (AP24534)1 Citation中文名: 帕纳替尼Target: VEGFR|PDGFR|Bcr-Abl|FGFR|SrcSummary: pan-BCR-ABL抑制剂,多激酶抑制剂
- A2133 Saracatinib (AZD0530)3 Citation中文名: 塞卡替尼Target: SrcSummary: Src/Abl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
- A2149 Bosutinib (SKI-606)1 Citation中文名: 伯舒替尼Target: Bcr-Abl|SrcSummary: Abl/Src有效的抑制剂
- A8215 PP 1Target: Src|EGFR|JAK|ZAP-70Summary: Src家族酪氨酸激酶抑制剂
- A3870 TG 100801Target: VEGFR|FGFR|Src|Fyn kinaseSummary: 多激酶抑制剂
- A3558 LRRK2-IN-11 CitationTarget: LRRK2|DCLK2Summary: LRRK2抑制剂