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

• Published in: Pharmaceutics Vol. 13; no. 11; p. 1748
• Main Authors: Kawano, Takahito, Inokuchi, Junichi, Eto, Masatoshi, Murata, Masaharu, Kang, Jeong-Hun
• Format: Journal Article
• Language: English
• Published: Basel MDPI AG 20-10-2021; MDPI
• Subjects: activator; Alzheimer's disease; Apoptosis; Binding sites; Cancer; Cell cycle; Cell growth; clinical trial; Clinical trials; Competition; Cyclin-dependent kinases; Glycoproteins; inhibitor; Kinases; Leukemia; Medical prognosis; Mutation; Phase transitions; Phosphorylation; protein kinase C; Proteins; Review; Signal transduction; signaling pathway; Tumors
• ISSN: 1999-4923; 1999-4923
• DOI: 10.3390/pharmaceutics13111748

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; α, βI, βII, and γ), novel or non-classic PKC isozymes (nPKCs; δ, ε, η, and θ), and atypical PKC isozymes (aPKCs; ζ, ι, and λ). 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.