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Título:
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The hard-to-close window of T-type calcium channels;
Targeting T-type channels
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Autor/a:
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Visa Pretel, Anna; Shaikh, Soni; Alza, Lía; Herreros Danés, Judit; Cantí Nicolás, Carles
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Notas:
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T-Type calcium channels (TTCCs) are key regulators of membrane excitability, which is the reason why TTCC pharmacology is subject to intensive research in the neurological and cardiovascular fields. TTCCs also play a role in cancer physiology, and pharmacological blockers such as tetralols and dihydroquinazolines (DHQs) reduce the viability of cancer cells in vitro and slow tumor growth in murine xenografts. However, the available compounds are better suited to blocking TTCCs in excitable membranes rather than TTCCs contributing window currents at steady potentials. Consistently, tetralols and dihydroquinazolines exhibit cytostatic/cytotoxic activities at higher concentrations than those required for TTCC blockade, which may involve off-target effects. Gene silencing experiments highlight the targetability of TTCCs, but further pharmacological research is required for TTCC blockade to become a chemotherapeutic option.
A.V. was the recipient of a predoctoral fellowship from the University of Lleida. S.S. was funded by the Marie Curie COFUND Programme. This work was supported by Instituto de Salud Carlos III/FEDER (PI13/01980 to J.H.). |
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Derechos:
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cc-by-nc-nd (c) Elsevier, 2019
http://creativecommons.org/licenses/by-nc-nd/4.0/
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Tipo de documento:
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Artículo
Artículo - Versión aceptada |
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Editor:
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Elsevier
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