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

ABSTRACT: 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.

SUBMITTER: Kawano T

PROVIDER: S-EPMC8621927 | biostudies-literature | 2021 Oct

REPOSITORIES: biostudies-literature

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

Kawano Takahito T Inokuchi Junichi J Eto Masatoshi M Murata Masaharu M Kang Jeong-Hun JH

Pharmaceutics 20211020 11

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-as ...[more]

PMID: 34834162

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