The In Vitro & In Vivo Pharmacology of Novel Tmem16a Potentiator Compounds – NACFC – Nashville – October 2019 Henry Danahay1,2, Sarah Lilley1, Holly Charlton1, Roy Fox1, Brian Button3, Juan Sabater4, Martin Gosling1,2 1University of Sussex, Brighton, UK; 2Enterprise Therapeutics, UK; 3University of North Carolina, Chapel Hill, USA; Mount Sinai Medical Center, Miami, USA TMEM16A […]

ECFS Clinical Meeting Liverpool TMEM16A potentiator Objectives: TMEM16A (ANO1) is a Ca2+-activated, alternative chloride channel expressed in the human airway epithelium. A potentiator of TMEM16A is predicted to enhance the secretion of chloride and thereby increase mucus hydration and clearance in the CF lung. Our aim is to discover and test the efficacy of novel […]

Something old and something new: ENaC & TMEM16A as targets to hydrate mucus in the CF airway Henry Danahay, Enterprise Therapeutics, Brighton, UK In the absence of functional CFTR in the apical membrane, the epithelial sodium channel (ENaC) and TMEM16A, a calcium activated chloride channel, are key regulators of airway mucosal hydration. As drug targets, […]

EACT increases intracellular calcium levels by a TMEM16A-independent mechanism Sarah Lilley1, Henry Danahay1,2, Holly Charlton1, Kathryn Adley1, Roy Fox1, Martin Gosling1,2 1University of Sussex, Brighton, UK; 2Enterprise Therapeutics, UK The N-aroylaminothiazole EACT was first described by Namkung et al. (2011) as an activator of the calcium-activated chloride channel, TMEM16A. Subsequently, EACT has been used as […]