The DOI matches its Crossref record; 9 of the 9 references it cites were found in a registry or an index.
Therapeutic targeting of 3′,5′-cyclic nucleotide phosphodiesterases: inhibition and beyond
Open accessAbstract
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. Cyclic nucleotide phosphodiesterases (PDEs) have roles in numerous biological processes and their dysfunction has been associated with various diseases including those affecting the nervous system, the cardiovascular system, fertility, immunity, cancer and metabolism. Here, Kelly and colleagues assess the current status of therapeutic PDE inhibitors, and highlight emerging novel strategies to therapeutically target PDE function.
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Metadata
- Authors
- Baillie, G. S., Tejeda, G. S., & Kelly, M. P.
- Venue
- Nature Reviews Drug Discovery
- Published
- 2019-08-06
- Volume
- 18
- Issue
- 10
- Pages
- 770-796
- ISSN
- 1474-1776 (ISSN-L)
- 1474-1784
- OpenAlex
- W2966771092
- Cited by
- 339
- References
- 9
- FWCI
- 2.53
- Type
- journal article
- Language
- en
- Open access
- green
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