Key result
Anthracene-9-carboxylic acid (A9C) acts as both an open channel blocker and a gating modifier of TMEM16A channels by binding to a region within the pore accessible from the extracellular side.
Population
Cloned TMEM16A channels and native calcium-activated chloride channels (CaCCs)
Design
Preclinical
Authors
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May inform TMEM16A modulator design; leaves open clinical translation from this animal model.
A9C acts as both an open channel blocker and gating modifier of TMEM16A channels, providing mechanistic insights for future drug design targeting calcium-activated chloride channels.
Ta et al. (2015) studied this question. Anthracene-9-carboxylic acid (A9C) vs. Absence of A9C was evaluated on TMEM16A channel activation and inhibition. Anthracene-9-carboxylic acid (A9C) acts as both an open channel blocker and a gating modifier of TMEM16A channels by binding to a region within the pore accessible from the extracellular side.
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