Transient receptor potential ankyrin 1 (TRPA1) modulators: Recent update and future perspective.
Agonists
Antagonists
Ion channel
TRPA1
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
05 Sep 2023
05 Sep 2023
Historique:
received:
29
01
2023
revised:
17
04
2023
accepted:
17
04
2023
medline:
19
6
2023
pubmed:
4
6
2023
entrez:
3
6
2023
Statut:
ppublish
Résumé
The transient receptor potential ankyrin 1 (TRPA1) channel is a non-selective cation channel that senses irritant chemicals. Its activation is closely associated with pain, inflammation, and pruritus. TRPA1 antagonists are promising treatments for these diseases, and there has been a recent upsurge in their application to new areas such as cancer, asthma, and Alzheimer's disease. However, due to the generally disappointing performance of TRPA1 antagonists in clinical studies, scientists must pursue the development of antagonists with higher selectivity, metabolic stability, and solubility. Moreover, TRPA1 agonists provide a deeper understanding of activation mechanisms and aid in antagonist screening. Therefore, we summarize the TRPA1 antagonists and agonists developed in recent years, with a particular focus on structure-activity relationships (SARs) and pharmacological activity. In this perspective, we endeavor to keep abreast of cutting-edge ideas and provide inspiration for the development of more effective TRPA1-modulating drugs.
Identifiants
pubmed: 37269667
pii: S0223-5234(23)00358-6
doi: 10.1016/j.ejmech.2023.115392
pii:
doi:
Substances chimiques
Transient Receptor Potential Channels
0
TRPA1 Cation Channel
0
Ankyrins
0
Cytoskeletal Proteins
0
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
115392Informations de copyright
Copyright © 2023. Published by Elsevier Masson SAS.
Déclaration de conflit d'intérêts
Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.