Activators and Inhibitors of Protein Kinase C (PKC): Their Applications in Clinical Trials

Protein kinase C (PKC), a family of phospholipid-dependent serine/threonine kinase, is classed into three subfamilies based on their structural and activation characteristics: conventional or classic PKC isozymes (cPKCs; alpha, beta I, beta II, and gamma), novel or non-classic PKC isozymes (nPKCs; delta, epsilon, eta, and theta), and atypical PKC isozymes (aPKCs; zeta, iota, and lambda). PKC inhibitors and activators are used to understand PKC-mediated intracellular signaling pathways and for the diagnosis and treatment of various PKC-associated diseases, such as cancers, neurological diseases, cardiovascular diseases, and infections. Many clinical trials of PKC inhibitors in cancers showed no significant clinical benefits, meaning that there is a limitation to design a cancer therapeutic strategy targeting PKC alone. This review will focus on the activators and inhibitors of PKC and their applications in clinical trials.

Automated summary

PKC is a family of important kinases classified into three subfamilies based on structural and activation characteristics, and used for understanding intracellular signaling pathways and treating related diseases. While PKC inhibitors in clinical trials for cancers did not show significant benefits, there is still potential for their application in research on other diseases.