Tyrosine Kinase - Cyclin-Dependent Kinases - Bcr-Abl
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.
- B2171 Imatinib (STI571)中文名: 伊马替尼Target: PDGFR|c-Kit|Bcr-AblSummary: 蛋白酪氨酸激酶抑制剂
- B1299 1-NM-PP1Target: Cyclin-Dependent Kinases|Bcr-Abl|Src|Ca2 /calmodulin-dependent protein kinases (CaMKs)|c-FynSummary: Pp60c-src抑制剂
- B1404 DCC-2036 (Rebastinib)Target: FLT3|Bcr-Abl|Tie-2|KDRSummary: Bcr-Abl抑制剂
- B1402 GZD824Target: Bcr-AblSummary: Bcr-Abl抑制剂
- A8812 PD173955Target: Bcr-Abl|SrcSummary: Src/Abl激酶双重抑制剂
- A8604 GNF 5Target: Bcr-AblSummary: Bcr-Abl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
- 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
- A1805 Imatinib Mesylate (STI571)中文名: 甲磺酸伊马替尼Target: PDGFR|c-Kit|Bcr-AblSummary: Abl/c-kit/PDGFR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