Sotrastaurin, a new selective protein kinase C inhibitor, on the way.

摘要

The protein kinase Cs (PKCs), a family of serine-/ threonine-specific protein kinases, are involved in diverse signal transduction pathways that modulate a wide variety of cellular events including activation, proliferation, differentiation, apoptosis, and autophagy. To date, at least 10 isotypes of PKCs are known. They are divided into three subfamilies according to their structure and type of activation: classical/conventional PKCs (cPKC: alpha, betaI-II, and gamma) are diacylglycerol (DAG) and calcium-dependent enzymes, and novel PKCs (nPKC: delta, epsilon, eta, and theta) that require DAG, but not calcium, for activation.