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Front Physiol. 2020 Nov 25;11:574030. doi: 10.3389/fphys.2020.574030. eCollection 2020.

Protein Kinase Inhibitor Peptide as a Tool to Specifically Inhibit Protein Kinase A.

Frontiers in physiology

Chong Liu, Ping Ke, Jingjing Zhang, Xiaoying Zhang, Xiongwen Chen

Affiliations

  1. Department of Pharmacology, Second Military Medical University, Shanghai, China.
  2. Cardiovascular Research Center, Temple University School of Medicine, Philadelphia, PA, United States.

PMID: 33324237 PMCID: PMC7723848 DOI: 10.3389/fphys.2020.574030

Abstract

The protein kinase enzyme family plays a pivotal role in almost every aspect of cellular function, including cellular metabolism, division, proliferation, transcription, movement, and survival. Protein kinase A (PKA), whose activation is triggered by cyclic adenosine monophosphate (cAMP), is widely distributed in various systems and tissues throughout the body and highly related to pathogenesis and progression of various kinds of diseases. The inhibition of PKA activation is essential for the study of PKA functions. Protein kinase inhibitor peptide (PKI) is a potent, heat-stable, and specific PKA inhibitor. It has been demonstrated that PKI can block PKA-mediated phosphorylase activation. Since then, researchers have a lot of knowledge about PKI. PKI is considered to be the most effective and specific method to inhibit PKA and is widely used in related research. In this review, we will first introduce the knowledge on the activation of PKA and mechanisms related on the inhibitory effects of PKI on PKA. Then, we will compare PKI-mediated PKA inhibition vs. several popular methods of PKA inhibition.

Copyright © 2020 Liu, Ke, Zhang, Zhang and Chen.

Keywords: H89; cyclic adenosine monophosphate; protein kinase A; protein kinase A inhibition; protein kinase inhibitor peptide

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