Abstract
TMEM16A, a calcium-activated chloride channel involved in multiple cellular processes, is a proposed target for diseases such as hypertension, asthma, and cystic fibrosis, but its pharmacology remains poorly understood. Here, we present a cryo-EM structure of TMEM16A in complex with the channel blocker 1PBC and a detailed functional analysis of its inhibition mechanism. A defined binding pocket located immediately external to the neck region of the hourglass-shaped pore is responsible for open-channel block by 1PBC and presumably chemically similar compounds.
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