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Issue 23, 2018
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Peptide-based development of PKA activators

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Protein kinases are among the most important regulators of cellular homeostasis, regulating many aspects of the cell life cycle through phosphorylation. The threonine/serine kinase cAMP-dependent protein kinase (PKA) is a major intracellular effector for a variety of bioactive molecules and hormones that work via a cAMP signaling pathway. In this work we report the discovery of a peptide and its simple peptidomimetic derivatives, which can activate the PKA catalytic unit. The direct binding of these new compounds to PKA and their resulting and activation mode were demonstrated by cellular (cardiomyocytes) and in vitro methods. Activation of PKA in cardiomyocytes after myocardial infarction might be a promising therapeutic strategy to protect the heart from ischemia and reperfusion. In addition, small-molecule PKA activators may prove useful as pharmacological tools for studying transduction mechanisms related to PKA. Several small molecules, which can activate a regulatory PKA unit, were developed. However, no small molecules that can activate a PKA catalytic unit were described in the scientific literature.

Graphical abstract: Peptide-based development of PKA activators

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Supplementary files

Article information

10 Apr 2018
09 Oct 2018
First published
17 Oct 2018

New J. Chem., 2018,42, 18585-18597
Article type

Peptide-based development of PKA activators

S. Kahremany, M. Zhenin, Y. Shenberger, D. Maimoun, G. Colotti, M. Arad, A. Shainberg, H. Senderowitz, S. Ruthstein and A. Gruzman, New J. Chem., 2018, 42, 18585
DOI: 10.1039/C8NJ01732H

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