PDE4 Inhibitors: Profiling Hits through the Multitude of Structural Classes

Article


Jian, J., Mazzacuva, F., Crocetti, L., Giovannoni, M. P. and Cilibrizzi, A. 2023. PDE4 Inhibitors: Profiling Hits through the Multitude of Structural Classes. International Journal of Molecular Sciences. 24 (14), p. 11518. https://doi.org/10.3390/ijms241411518
AuthorsJian, J., Mazzacuva, F., Crocetti, L., Giovannoni, M. P. and Cilibrizzi, A.
Abstract

Cyclic nucleotide phosphodiesterases 4 (PDE4) are a family of enzymes which specifically promote the hydrolysis and degradation of cAMP. The inhibition of PDE4 enzymes has been widely investigated as a possible alternative strategy for the treatment of a variety of respiratory diseases, including chronic obstructive pulmonary disease and asthma, as well as psoriasis and other autoimmune disorders. In this context, the identification of new molecules as PDE4 inhibitors continues to be an active field of investigation within drug discovery. This review summarizes the medicinal chemistry journey in the design and development of effective PDE4 inhibitors, analyzed through chemical classes and taking into consideration structural aspects and binding properties, as well as inhibitory efficacy, PDE4 selectivity and the potential as therapeutic agents.

JournalInternational Journal of Molecular Sciences
Journal citation24 (14), p. 11518
ISSN1422-0067
Year2023
PublisherMDPI
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Anyone
Digital Object Identifier (DOI)https://doi.org/10.3390/ijms241411518
Publication dates
Online15 Jul 2023
Publication process dates
Accepted13 Jul 2023
Deposited22 Feb 2024
Copyright holder© 2023, The Authors
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