ArticleCells2025
Tranilast Does Not Inhibit TRPV2.
Article in Cells, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Authors and funding
5 authors.
Funding
Abstract
Transient receptor potential vanilloid 2 (TRPV2) is a non-selective cation channel involved in diverse physiological and pathological processes. Tranilast has frequently been described and used as a rather specific inhibitor of TRPV2. However, the molecular basis of this inhibition was never been studied in detail. Here, we investigated whether tranilast indeed directly inhibits TRPV2. Rat TRPV2 was expressed in human embryonic kidney (HEK293) cells, and channel function was assessed using whole-cell electrophysiology and calcium imaging in response to established agonists. In parallel, we conducted phagocytosis assays in rat basophilic leukemia (RBL) cells, including a CRISPR/Cas9-generated TRPV2-knockout cell line. Tranilast up to 1 mM did not inhibit TRPV2-mediated currents or calcium influx induced by any agonist. However, when co-applied with the oxidant chloramine T, tranilast diminished oxidation-induced activation of TRPV2. This effect may indicate a general interference of tranilast with redox signaling. Accordingly, tranilast also reduced chloramine T-induced activation of TRPA1 as well as the development of non-inactivating currents of voltage-gated Na
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