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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...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2023
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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. |
format | Online Article Text |
id | pubmed-10380597 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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