Calcium-activated chloride channel TMEM16A (TMEM16A (also known as ANO1 or anoctamin-1))

Calcium-activated chloride channel TMEM16A is a transmembrane protein that forms a homodimeric ion channel, selectively conducting chloride ions across cell membranes in response to increased intracellular calcium levels[2][3][5][9][10]. TMEM16A is broadly expressed in epithelial tissues, smooth muscle, and neurons, mediating biological functions such as epithelial fluid secretion, smooth muscle contraction, and regulation of neuronal excitability[1][4][5]. The channel is involved in several physiological and pathological processes, including control of airway and exocrine gland secretion, rhythmic contractions in the gastrointestinal tract, regulation of blood pressure, and some forms of pain signaling (nociception)[1][5][7]. Overactivation or dysregulation of TMEM16A has been implicated in diseases including cancer, asthma, hypertension, and gastrointestinal motility disorders, making it an emerging therapeutic target, especially for conditions related to abnormal chloride secretion or smooth muscle function[10]. TMEM16A gating is regulated by direct binding of calcium to specific conserved sites in the transmembrane region; pharmacological inhibitors targeting TMEM16A are under investigation for their potential clinical applications[1][6][7][10].

Other names

Anoctamin-1ANO1TMEM16ACalcium-activated chloride channelCaCC

Inhibition of chloride ion conductance via blockade of channel pore; Modulation of channel gating by altering Ca2+ sensitivity or channel conformation; Allosteric interaction with channel accessory regulators (e.g., targeting PIP2-binding site)[7]