Src Inhibitors

Src kinase which associates with various intracellular membranes, where it catalyzes the transfer of phosphate from ATP to a tyrosine residue within proteins is an non-receptor class of tyrosine kinases including Src, Fyn, Yes, Fgr, Hck, Lyn, Lck and Blk. Src plays an important role in both receptor-tyrosine-kinase-mediated proliferation and transformation of the cell to a tumor phenotype. Src is phosphorylated and activated by the growth factors binding to growth factor receptors including VEGFR, PDGFR, c-met receptors, ErbB family receptors and interleukin 6 (IL-6) receptors. Activated Src transduces a signal via phosphorylation of the adaptor protein Shc to the cascade that involves Ras and the mitogen-activated protein kinase (MAPK) family member, extracellular regulated kinase (Erk). This induces transcription of the early gene c-myc and increases DNA synthesis. Src can activate signal transducer and activator of transcription 3 (STAT3) via Src and Erk kinase and induce cell transformation.