T-type Calcium Channels in Health and Disease.
T-type calcium channels
channel function
modulators
pathophysiological roles
rational drug design
structural determinants.
Journal
Current medicinal chemistry
ISSN: 1875-533X
Titre abrégé: Curr Med Chem
Pays: United Arab Emirates
ID NLM: 9440157
Informations de publication
Date de publication:
2020
2020
Historique:
received:
06
07
2018
revised:
28
08
2018
accepted:
30
08
2018
pubmed:
3
10
2018
medline:
6
8
2020
entrez:
3
10
2018
Statut:
ppublish
Résumé
Low Voltage-Activated (LVA) T-type calcium channels are characterized by transient current and Low Threshold Spikes (LTS) that trigger neuronal firing and oscillatory behavior. Combined with their preferential localization in dendrites and their specific "window current", T-type calcium channels are considered to be key players in signal amplification and synaptic integration. Assisted by the emerging pharmacological tools, the structural determinants of channel gating and kinetics, as well as novel physiological and pathological functions of T-type calcium channels, are being uncovered. In this review, we provide an overview of structural determinants in T-type calcium channels, their involvement in disorders and diseases, the development of novel channel modulators, as well as Structure-Activity Relationship (SAR) studies that lead to rational drug design.
Identifiants
pubmed: 30277145
pii: CMC-EPUB-93312
doi: 10.2174/0929867325666181001112821
doi:
Substances chimiques
Calcium Channel Blockers
0
Calcium Channels, T-Type
0
Calcium
SY7Q814VUP
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
3098-3122Informations de copyright
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