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PDE4 Inhibitors: Profiling Hits through the Multitude of Structural Classes

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 ch...

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Detalles Bibliográficos
Autores principales: Jin, Jian, Mazzacuva, Francesca, Crocetti, Letizia, Giovannoni, Maria Paola, Cilibrizzi, Agostino
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10380597/
https://www.ncbi.nlm.nih.gov/pubmed/37511275
http://dx.doi.org/10.3390/ijms241411518
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author Jin, Jian
Mazzacuva, Francesca
Crocetti, Letizia
Giovannoni, Maria Paola
Cilibrizzi, Agostino
author_facet Jin, Jian
Mazzacuva, Francesca
Crocetti, Letizia
Giovannoni, Maria Paola
Cilibrizzi, Agostino
author_sort Jin, Jian
collection PubMed
description 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.
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spelling pubmed-103805972023-07-29 PDE4 Inhibitors: Profiling Hits through the Multitude of Structural Classes Jin, Jian Mazzacuva, Francesca Crocetti, Letizia Giovannoni, Maria Paola Cilibrizzi, Agostino Int J Mol Sci Review 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. MDPI 2023-07-15 /pmc/articles/PMC10380597/ /pubmed/37511275 http://dx.doi.org/10.3390/ijms241411518 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Jin, Jian
Mazzacuva, Francesca
Crocetti, Letizia
Giovannoni, Maria Paola
Cilibrizzi, Agostino
PDE4 Inhibitors: Profiling Hits through the Multitude of Structural Classes
title PDE4 Inhibitors: Profiling Hits through the Multitude of Structural Classes
title_full PDE4 Inhibitors: Profiling Hits through the Multitude of Structural Classes
title_fullStr PDE4 Inhibitors: Profiling Hits through the Multitude of Structural Classes
title_full_unstemmed PDE4 Inhibitors: Profiling Hits through the Multitude of Structural Classes
title_short PDE4 Inhibitors: Profiling Hits through the Multitude of Structural Classes
title_sort pde4 inhibitors: profiling hits through the multitude of structural classes
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10380597/
https://www.ncbi.nlm.nih.gov/pubmed/37511275
http://dx.doi.org/10.3390/ijms241411518
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