PDE4 Inhibitors: Profiling Hits through the Multitude of Structural Classes

Jian Jin, Francesca Mazzacuva, Letizia Crocetti, Maria Paola Giovannoni, Agostino Cilibrizzi

Research output: Contribution to journalReview articlepeer-review

5 Citations (SciVal)

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.

Original languageEnglish
Article number11518
JournalInternational Journal of Molecular Sciences
Volume24
Issue number14
DOIs
Publication statusPublished - 15 Jul 2023
Externally publishedYes

Bibliographical note

Funding
This research received no external funding.

Data Availability Statement
Not applicable.

Keywords

  • dual activity
  • PDE4 inhibitors
  • PDE4 selectivity
  • phosphodiesterases 4
  • respiratory diseases
  • structural analysis

ASJC Scopus subject areas

  • Catalysis
  • Molecular Biology
  • Spectroscopy
  • Computer Science Applications
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Inorganic Chemistry

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