TMEM16A inhibitors reveal TMEM16A as a minor component of calcium-activated chloride channel conductance in airway and intestinal epithelial cells
W Namkung, PW Phuan, AS Verkman - Journal of Biological Chemistry, 2011 - jbc.org
TMEM16A (ANO1) functions as a calcium-activated chloride channel (CaCC). We
developed pharmacological tools to investigate the contribution of TMEM16A to CaCC
conductance in human airway and intestinal epithelial cells. A screen of∼ 110,000
compounds revealed four novel chemical classes of small molecule TMEM16A inhibitors
that fully blocked TMEM16A chloride current with an IC 50< 10 μm, without interfering with
calcium signaling. Following structure-activity analysis, the most potent inhibitor, an …
developed pharmacological tools to investigate the contribution of TMEM16A to CaCC
conductance in human airway and intestinal epithelial cells. A screen of∼ 110,000
compounds revealed four novel chemical classes of small molecule TMEM16A inhibitors
that fully blocked TMEM16A chloride current with an IC 50< 10 μm, without interfering with
calcium signaling. Following structure-activity analysis, the most potent inhibitor, an …
