Identification and Characterization of Synthetic Peptide Substrates and Small Molecule Inhibitors of Non Receptor Tyrosine Kinase Etk

摘要

Etk is a member of the Btk family of tyrosine kinases that has a modular structure consisting of N-terminal PH domain, SH3, SH2, and C-terminal catalytic domain . First identified in LNCaP prostate cancer cells, Etk is widely expressed in hematopoietic, epithelial, and endothelial cells. Previous studies show that Etk is involved in several networks of signaling cascades through its PH domain. So far Etk is considered to be a downstream effector of phosphatidylinositol 3'-kinase (PI3-kinase) during interleukin 6 (IL-6) induced neuroendocrine differentiation, PI3 kinase and upstream signaling molecule of Pakl (p21 activator kinase) in cell proliferation and anchorage dependent growth pathway. In other studies, Etk has been demonstrated to function as a link between Src and STAT3. Taken together, Etk is involved in a network of complicated signaling pathways with possible overlapping upstream and downstream effectors.