Mibefradil, a T-type Ca
Calcium
/ analysis
Calcium Channel Blockers
/ chemistry
Calcium Channels
/ metabolism
Cell Death
/ drug effects
Cell Proliferation
/ drug effects
Cells, Cultured
HEK293 Cells
Humans
Mibefradil
/ chemistry
ORAI1 Protein
/ antagonists & inhibitors
ORAI2 Protein
/ antagonists & inhibitors
Optical Imaging
Journal
British journal of pharmacology
ISSN: 1476-5381
Titre abrégé: Br J Pharmacol
Pays: England
ID NLM: 7502536
Informations de publication
Date de publication:
10 2019
10 2019
Historique:
received:
29
10
2018
revised:
21
06
2019
accepted:
28
06
2019
pubmed:
5
7
2019
medline:
22
9
2020
entrez:
5
7
2019
Statut:
ppublish
Résumé
Mibefradil, a T-type Ca Human Orai1-3 cDNAs in tetracycline-regulated pcDNA4/TO vectors were transfected into HEK293 T-REx cells with stromal interaction molecule 1 (STIM1) stable expression. The Orai currents were recorded by whole-cell and excised-membrane patch clamp. Ca Mibefradil inhibited Orai1, Orai2, and Orai3 currents dose-dependently. The IC Mibefradil is a potent cell surface blocker of Orai channels, demonstrating a new pharmacological action of this compound in regulating cell growth and death, which could be relevant to its anti-cancer activity.
Sections du résumé
BACKGROUND AND PURPOSE
Mibefradil, a T-type Ca
EXPERIMENTAL APPROACH
Human Orai1-3 cDNAs in tetracycline-regulated pcDNA4/TO vectors were transfected into HEK293 T-REx cells with stromal interaction molecule 1 (STIM1) stable expression. The Orai currents were recorded by whole-cell and excised-membrane patch clamp. Ca
KEY RESULTS
Mibefradil inhibited Orai1, Orai2, and Orai3 currents dose-dependently. The IC
CONCLUSIONS AND IMPLICATIONS
Mibefradil is a potent cell surface blocker of Orai channels, demonstrating a new pharmacological action of this compound in regulating cell growth and death, which could be relevant to its anti-cancer activity.
Identifiants
pubmed: 31271653
doi: 10.1111/bph.14788
pmc: PMC6780027
doi:
Substances chimiques
Calcium Channel Blockers
0
Calcium Channels
0
ORAI1 Protein
0
ORAI1 protein, human
0
ORAI2 Protein
0
ORAI2 protein, human
0
Orai3 protein, human
0
Mibefradil
27B90X776A
Calcium
SY7Q814VUP
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
3845-3856Informations de copyright
© 2019 The British Pharmacological Society.
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