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Int. J. Mol. Sci. 2016, 17(10), 1672; doi:10.3390/ijms17101672

Modulation of Compartmentalised Cyclic Nucleotide Signalling via Local Inhibition of Phosphodiesterase Activity

Department of Physiology, Anatomy and Genetics, University of Oxford, Oxford OX1 3TP, UK
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Author to whom correspondence should be addressed.
Academic Editor: Claudiu T. Supuran
Received: 15 July 2016 / Revised: 20 September 2016 / Accepted: 23 September 2016 / Published: 2 October 2016
(This article belongs to the Special Issue Enzyme-Inhibitor Interaction as Examples of Molecular Recognition)
View Full-Text   |   Download PDF [661 KB, uploaded 2 October 2016]   |  

Abstract

Cyclic nucleotide phosphodiesterases (PDEs) are the only enzymes that degrade the cyclic nucleotides cAMP and cGMP, and play a key role in modulating the amplitude and duration of the signal delivered by these two key intracellular second messengers. Defects in cyclic nucleotide signalling are known to be involved in several pathologies. As a consequence, PDEs have long been recognized as potential drug targets, and they have been the focus of intense research for the development of therapeutic agents. A number of PDE inhibitors are currently available for the treatment of disease, including obstructive pulmonary disease, erectile dysfunction, and heart failure. However, the performance of these drugs is not always satisfactory, due to a lack of PDE-isoform specificity and their consequent adverse side effects. Recent advances in our understanding of compartmentalised cyclic nucleotide signalling and the role of PDEs in local regulation of cAMP and cGMP signals offers the opportunity for the development of novel strategies for therapeutic intervention that may overcome the current limitation of conventional PDE inhibitors. View Full-Text
Keywords: cAMP; cGMP; Compartmentalisation; Phosphodiesterases (PDEs); PDE inhibitor; protein kinase A; signaling cAMP; cGMP; Compartmentalisation; Phosphodiesterases (PDEs); PDE inhibitor; protein kinase A; signaling
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Brescia, M.; Zaccolo, M. Modulation of Compartmentalised Cyclic Nucleotide Signalling via Local Inhibition of Phosphodiesterase Activity. Int. J. Mol. Sci. 2016, 17, 1672.

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