Association of TMEM16A
chloride channel overexpression with airway goblet cell metaplasia.
The therapies target the ion channels TMEM16A
and ENaC with the aim of increasing hydration and clearing mucus.
Goepp et al., "Proinflammatory cytokine secretion is suppressed by TMEM16A
or CFTR channel activity in human cystic fibrosis bronchial epithelia," Molecular Biology of the Cell, vol.
Although 9-phenanthrol was initially discovered as an inhibitor of the TRPM4 channels, later studies showed that it also inhibits the transmembrane protein 16A (TMEM16A), a [Ca.sup.2+]-activated [Cl.sup.-] channel .
have recently demonstrated that chloride efflux through a [Ca.sup.2+]-activated [Cl.sup.-] channel, anoctamine 1 (Ano1), also called "transmembrane member 16A" (TMEM16A), is involved in mediating the glucose-stimulated insulin secretion .
We have demonstrated that 9-phenanthrol, an inhibitor of the TRPM4 and the TMEM16A channels and an activator of the [K.sub.ca]3.1 channel, strongly inhibits both the glucose-and the GLP-1-induced insulin secretion.
DOG1 is also known as Anoctamin-1 (Ano-1), transmembrane protein 16A (TMEM16A), overexpressed in oral (squamous cell) carcinoma 2 (ORAOV2), and tumor-amplified and overexpressed sequence 1 (TAOS1).
TMEM16A confers receptor-activated calcium-dependent chloride conductance.
TMEM16A, a membrane protein associated with calcium-dependent chloride channel activity.
Rock and his colleagues focused on a calcium-activated chloride channel called TMEM16A. This channel secretes chloride ions in response to rises in intracellular calcium.
Step two consisted of a screen to identify chemicals that inhibit the activity of TMEM16A. The authors identified three chemicals that inhibit the channel.
It is also known as FLJ10261 (hypothetic gene product that was unofficially called DOG1), TMEM16A
(transmembrane protein 16A), or ANO1 (anoctamin 1, calcium-activated chloride channel); DOG1 being the most well-accepted name in the diagnostic literature.