Baillie, G. S. , Tejeda, G. S. and Kelly, M. P. (2019) Therapeutic targeting of 3’,5’-cyclic nucleotide phosphodiesterases: inhibition and beyond. Nature Reviews Drug Discovery, 18, pp. 770-796. (doi: 10.1038/s41573-019-0033-4) (PMID:31388135)
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Abstract
Phosphodiesterases (PDEs), enzymes that degrade 3′,5′-cyclic nucleotides, are being pursued as therapeutic targets for several diseases, including those affecting the nervous system, the cardiovascular system, fertility, immunity, cancer and metabolism. Clinical development programmes have focused exclusively on catalytic inhibition, which continues to be a strong focus of ongoing drug discovery efforts. However, emerging evidence supports novel strategies to therapeutically target PDE function, including enhancing catalytic activity, normalizing altered compartmentalization and modulating post-translational modifications, as well as the potential use of PDEs as disease biomarkers. Importantly, a more refined appreciation of the intramolecular mechanisms regulating PDE function and trafficking is emerging, making these pioneering drug discovery efforts tractable.
| Item Type: | Articles |
|---|---|
| Status: | Published |
| Refereed: | Yes |
| Glasgow Author(s) Enlighten ID: | Tejeda, Dr Gonzalo and Baillie, Professor George |
| Authors: | Baillie, G. S., Tejeda, G. S., and Kelly, M. P. |
| College/School: | College of Medical Veterinary and Life Sciences > School of Cardiovascular & Metabolic Health |
| Journal Name: | Nature Reviews Drug Discovery |
| Publisher: | Nature Research |
| ISSN: | 1474-1776 |
| ISSN (Online): | 1474-1784 |
| Published Online: | 06 August 2019 |
| Copyright Holders: | Copyright © 2019 Springer Nature |
| First Published: | First published in Nature Reviews Drug Discovery 18:770-796 |
| Publisher Policy: | Reproduced in accordance with the publisher copyright policy |
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