Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent.

摘要: CGP 41251 was originally identified as an inhibitor of protein kinase C (PKC), inhibiting mainly the conventional PKC subtypes, and subsequently shown to inhibit vascular endothelial growth factor (VEGF) receptor insert domain-containing receptor, which is involved in angiogenesis. inhibits reversibly intracellular activity, induction c-fos corresponding activation mitogen-activated induced by either tumor promoting phorbol esters, platelet-derived factor, or basic fibroblast but not epidermal factor. inhibited ligand-induced autophosphorylation receptors for stem cell VEGF (kinase receptor) that correlated with inhibition activation, did affect insulin, insulin-like factor-I, showed broad antiproliferative activity against various normal lines vitro, able reverse p-glycoprotein-mediated multidrug resistance cells vitro. vivo antitumor single agent angiogenesis vivo. Thus, may suppress (via its effects on tyrosine kinases) addition directly proliferation PKCs).