[HTML][HTML] Potent and selective disruption of protein kinase D functionality by a benzoxoloazepinolone

ER Sharlow, KV Giridhar, CR LaValle, J Chen… - Journal of biological …, 2008 - ASBMB
Protein kinase D (PKD) is a novel family of serine/threonine kinases targeted by the second
messenger diacylglycerol. It has been implicated in many important cellular processes and
pathological conditions. However, further analysis of PKD in these processes is severely
hampered by the lack of a PKD-specific inhibitor that can be readily applied to cells and in
animal models. We now report the discovery of the first potent and selective cell-active small
molecule inhibitor for PKD, benzoxoloazepinolone (CID755673). This inhibitor was …