Activators and inhibitors of protein kinase c (Pkc): Their applications in clinical trials

Takahito Kawano, Junichi Inokuchi, Masatoshi Eto, Masaharu Murata, Jeong Hun Kang

Research output: Contribution to journalReview articlepeer-review

36 Citations (Scopus)


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.

Original languageEnglish
Article number1748
Issue number11
Publication statusPublished - Nov 2021

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science


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