The VRAC blocker DCPIB directly gates the BK channels and increases intracellular Ca

calcium-activated potassium channel intracellular calcium melanoma pancreatic duct adenocarcinoma potassium channel openers volume regulated anion channel

Journal

British journal of pharmacology
ISSN: 1476-5381
Titre abrégé: Br J Pharmacol
Pays: England
ID NLM: 7502536

Informations de publication

Date de publication:
07 2022
Historique:
revised: 18 01 2022
received: 30 03 2021
accepted: 24 01 2022
pubmed: 2 2 2022
medline: 10 6 2022
entrez: 1 2 2022
Statut: ppublish

Résumé

The volume regulated anion channel (VRAC) is known to be involved in different aspects of cancer cell behaviour and response to therapies. For this reason, we investigated the effect of DCPIB, a presumably specific blocker of VRAC, in two types of cancer: pancreatic duct adenocarcinoma (PDAC) and melanoma. We used patch-clamp electrophysiology, supported by Ca DCPIB markedly increased whole-cell currents in Panc-1, MiaPaca2 and IGR39, but not in IGR37 cells. The currents were mostly mediated by K DCPIB directly targeted BK channels and, also, acutely increased intracellular Ca

Sections du résumé

BACKGROUND AND PURPOSE
The volume regulated anion channel (VRAC) is known to be involved in different aspects of cancer cell behaviour and response to therapies. For this reason, we investigated the effect of DCPIB, a presumably specific blocker of VRAC, in two types of cancer: pancreatic duct adenocarcinoma (PDAC) and melanoma.
EXPERIMENTAL APPROACH
We used patch-clamp electrophysiology, supported by Ca
KEY RESULTS
DCPIB markedly increased whole-cell currents in Panc-1, MiaPaca2 and IGR39, but not in IGR37 cells. The currents were mostly mediated by K
CONCLUSION AND IMPLICATIONS
DCPIB directly targeted BK channels and, also, acutely increased intracellular Ca

Identifiants

pubmed: 35102550
doi: 10.1111/bph.15810
doi:

Substances chimiques

Anions 0
Large-Conductance Calcium-Activated Potassium Channels 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

3452-3469

Informations de copyright

© 2022 The British Pharmacological Society.

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Auteurs

Paolo Zuccolini (P)

Institute of Biophysics, National Research Council, Genoa, Italy.

Loretta Ferrera (L)

Institute of Biophysics, National Research Council, Genoa, Italy.
U.O.C. Genetica Medica, Istituto di Ricovero e Cura a Carattere Scientifico (IRCCS), Istituto Giannina Gaslini, Genoa, Italy.

Alessia Remigante (A)

Institute of Biophysics, National Research Council, Genoa, Italy.

Cristiana Picco (C)

Institute of Biophysics, National Research Council, Genoa, Italy.

Raffaella Barbieri (R)

Institute of Biophysics, National Research Council, Genoa, Italy.

Sara Bertelli (S)

Institute of Biophysics, National Research Council, Genoa, Italy.

Oscar Moran (O)

Institute of Biophysics, National Research Council, Genoa, Italy.

Paola Gavazzo (P)

Institute of Biophysics, National Research Council, Genoa, Italy.

Michael Pusch (M)

Institute of Biophysics, National Research Council, Genoa, Italy.

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