A sensitive, time-resolved fluorometric assay for detection of inhibitors of phosphotyrosine kinases

摘要

Phosphotyrosine kinases are involved in a variety of biological processes. These enzymes catalyze the transfer of orthophosphate from adenotriphosphate (ATP) to a protein acceptor. Alterations in their expression or activity are known to result in the initiation or progression of numerous types of cancer? A major therapeutic strategy has been to identify potent and selective low-molecular-weight inhibitors of phosphotyrosine kinases that may slow or stop the growth of tumor cells. In order to expedite the identification of such inhibitors, it is necessary to screen large numbers of compounds in a reliable, safe, and cost-effective manner.