Transmembrane protein 16A calcium-activated chloride channel (TMEM16A)

Transmembrane protein 16A calcium-activated chloride channel (TMEM16A) is a widely expressed, dimeric ion channel that is directly activated by increases in intracellular calcium, coupling cellular calcium signals to chloride ion flux across membranes[1][7][10]. TMEM16A plays essential roles in regulating epithelial fluid and mucous secretion, airway hydration, smooth and gastrointestinal muscle contractility, neuronal excitability, and sensory transduction[2][3][4][6][7][8][9]. Dysfunction or overexpression of TMEM16A is implicated in diseases such as asthma, cystic fibrosis, hypertension, inflammatory disorders, and several cancers, notably as a driver in some gastrointestinal stromal tumors[4][5][9]. The protein’s structure features two identical subunits, each forming a chloride conducting pore gated by calcium binding; it is subject to regulation by membrane lipids, phosphorylation, and protein-protein interactions[1][2][5][10]. Due to its contributions to various physiological processes and disease mechanisms, TMEM16A is considered a promising but challenging therapeutic target for drug development[5].

Other names

Anoctamin-1Ano1Calcium-activated chloride channel 1CaCCTransmembrane protein 16ATMEM16A channel

Inhibition of chloride channel function (inhibitors) Activation of chloride channel function (activators)