Advances in TRP channel drug discovery: from target validation to clinical studies.
Journal
Nature reviews. Drug discovery
ISSN: 1474-1784
Titre abrégé: Nat Rev Drug Discov
Pays: England
ID NLM: 101124171
Informations de publication
Date de publication:
01 2022
01 2022
Historique:
accepted:
07
07
2021
pubmed:
17
9
2021
medline:
4
2
2022
entrez:
16
9
2021
Statut:
ppublish
Résumé
Transient receptor potential (TRP) channels are multifunctional signalling molecules with many roles in sensory perception and cellular physiology. Therefore, it is not surprising that TRP channels have been implicated in numerous diseases, including hereditary disorders caused by defects in genes encoding TRP channels (TRP channelopathies). Most TRP channels are located at the cell surface, which makes them generally accessible drug targets. Early drug discovery efforts to target TRP channels focused on pain, but as our knowledge of TRP channels and their role in health and disease has grown, these efforts have expanded into new clinical indications, ranging from respiratory disorders through neurological and psychiatric diseases to diabetes and cancer. In this Review, we discuss recent findings in TRP channel structural biology that can affect both drug development and clinical indications. We also discuss the clinical promise of novel TRP channel modulators, aimed at both established and emerging targets. Last, we address the challenges that these compounds may face in clinical practice, including the need for carefully targeted approaches to minimize potential side-effects due to the multifunctional roles of TRP channels.
Identifiants
pubmed: 34526696
doi: 10.1038/s41573-021-00268-4
pii: 10.1038/s41573-021-00268-4
pmc: PMC8442523
doi:
Substances chimiques
Transient Receptor Potential Channels
0
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
41-59Subventions
Organisme : NIDCD NIH HHS
ID : R21 DC018497
Pays : United States
Informations de copyright
© 2021. Springer Nature Limited.
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