Click here to close
Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly.
We suggest using a current version of Chrome,
FireFox, or Safari.
Biochem Biophys Rep
2021 Dec 02;28:101180. doi: 10.1016/j.bbrep.2021.101180.
Show Gene links
Show Anatomy links
Positive modulation of the TMEM16B mediated currents by TRPV4 antagonist.
Hernandez A
,
Alaniz-Palacios A
,
Contreras-Vite JA
,
Martínez-Torres A
.
???displayArticle.abstract???
Calcium-activated chloride channels (CaCCs) play important roles in many physiological processes and their malfunction is implicated in diverse pathologies such as cancer, asthma, and hypertension. TMEM16A and TMEM16B proteins are the structural components of the CaCCs. Recent studies in cell cultures and animal models have demonstrated that pharmacological inhibition of CaCCs could be helpful in the treatment of some diseases, however, there are few specific modulators of these channels. CaCCs and Transient Receptor Potential Vanilloid-4 (TRPV4) channels are co-expressed in some tissues where they functionally interact. TRPV4 is activated by different stimuli and forms a calcium permeable channel that is activated by GSK1016790A and antagonized by GSK2193874. Here we report that GSK2193874 enhances the chloride currents mediated by TMEM16B expressed in HEK cells at nanomolar concentrations and that GSK1016790A enhances native CaCCs of Xenopus oocytes. Thus, these compounds may be used as a tool for the study of CaCCs, TRPV4 and their interactions.
André,
Axotomy-induced expression of calcium-activated chloride current in subpopulations of mouse dorsal root ganglion neurons.
2003, Pubmed
André,
Axotomy-induced expression of calcium-activated chloride current in subpopulations of mouse dorsal root ganglion neurons.
2003,
Pubmed
Angermann,
Mechanism of the inhibition of Ca2+-activated Cl- currents by phosphorylation in pulmonary arterial smooth muscle cells.
2006,
Pubmed
Barish,
A transient calcium-dependent chloride current in the immature Xenopus oocyte.
1983,
Pubmed
,
Xenbase
Britschgi,
Calcium-activated chloride channel ANO1 promotes breast cancer progression by activating EGFR and CAMK signaling.
2013,
Pubmed
Caputo,
TMEM16A, a membrane protein associated with calcium-dependent chloride channel activity.
2008,
Pubmed
Cho,
The calcium-activated chloride channel anoctamin 1 acts as a heat sensor in nociceptive neurons.
2012,
Pubmed
Contreras-Vite,
Revealing the activation pathway for TMEM16A chloride channels from macroscopic currents and kinetic models.
2016,
Pubmed
Crottès,
The multifaceted role of TMEM16A in cancer.
2019,
Pubmed
Cruz-Rangel,
Gating modes of calcium-activated chloride channels TMEM16A and TMEM16B.
2015,
Pubmed
Cruz-Rangel,
Extracellular protons enable activation of the calcium-dependent chloride channel TMEM16A.
2017,
Pubmed
Dang,
Cryo-EM structures of the TMEM16A calcium-activated chloride channel.
2017,
Pubmed
Davis,
Potent vasorelaxant activity of the TMEM16A inhibitor T16A(inh) -A01.
2013,
Pubmed
De Jesús-Pérez,
Phosphatidylinositol 4,5-bisphosphate, cholesterol, and fatty acids modulate the calcium-activated chloride channel TMEM16A (ANO1).
2018,
Pubmed
De La Fuente,
Small-molecule screen identifies inhibitors of a human intestinal calcium-activated chloride channel.
2008,
Pubmed
Doughty,
Non-specificity of chloride channel blockers in rat cerebral arteries: block of the L-type calcium channel.
1998,
Pubmed
Duvvuri,
TMEM16A induces MAPK and contributes directly to tumorigenesis and cancer progression.
2012,
Pubmed
Genovese,
TRPV4 and purinergic receptor signalling pathways are separately linked in airway epithelia to CFTR and TMEM16A chloride channels.
2019,
Pubmed
Gradogna,
Molecular Pharmacology of Kidney and Inner Ear CLC-K Chloride Channels.
2010,
Pubmed
Guinamard,
Flufenamic acid as an ion channel modulator.
2013,
Pubmed
Guo,
Calcium-activated chloride current contributes to action potential alternations in left ventricular hypertrophy rabbit.
2008,
Pubmed
Güler,
Heat-evoked activation of the ion channel, TRPV4.
2002,
Pubmed
,
Xenbase
Hartzell,
Calcium-activated chloride channels.
2005,
Pubmed
Hogg,
Effects of Cl channel blockers on Ca-activated chloride and potassium currents in smooth muscle cells from rabbit portal vein.
1994,
Pubmed
Hu,
Activation of TRPA1 channels by fenamate nonsteroidal anti-inflammatory drugs.
2010,
Pubmed
,
Xenbase
Huang,
Calcium-activated chloride channel TMEM16A modulates mucin secretion and airway smooth muscle contraction.
2012,
Pubmed
Keckeis,
Anoctamin2 (TMEM16B) forms the Ca2+-activated Cl- channel in the retinal pigment epithelium.
2017,
Pubmed
Kunzelmann,
Calcium-dependent chloride conductance in epithelia: is there a contribution by Bestrophin?
2007,
Pubmed
Lalonde,
Calcium-activated chloride channels in the retina.
2008,
Pubmed
,
Xenbase
Liu,
Eact, a small molecule activator of TMEM16A, activates TRPV1 and elicits pain- and itch-related behaviours.
2016,
Pubmed
Loukin,
Forward genetic analysis reveals multiple gating mechanisms of TRPV4.
2010,
Pubmed
,
Xenbase
Ma,
TMEM16A Contributes to Endothelial Dysfunction by Facilitating Nox2 NADPH Oxidase-Derived Reactive Oxygen Species Generation in Hypertension.
2017,
Pubmed
Matthews,
Calcium, the two-faced messenger of olfactory transduction and adaptation.
2003,
Pubmed
Miledi,
A calcium-dependent transient outward current in Xenopus laevis oocytes.
1982,
Pubmed
,
Xenbase
Namkung,
TMEM16A inhibitors reveal TMEM16A as a minor component of calcium-activated chloride channel conductance in airway and intestinal epithelial cells.
2011,
Pubmed
Oh,
Cellular functions of TMEM16/anoctamin.
2016,
Pubmed
Oh,
MONNA, a potent and selective blocker for transmembrane protein with unknown function 16/anoctamin-1.
2013,
Pubmed
,
Xenbase
Paulino,
Activation mechanism of the calcium-activated chloride channel TMEM16A revealed by cryo-EM.
2017,
Pubmed
Pifferi,
TMEM16B induces chloride currents activated by calcium in mammalian cells.
2009,
Pubmed
Qu,
The Ca(2+) -activated Cl(-) channel, ANO1 (TMEM16A), is a double-edged sword in cell proliferation and tumorigenesis.
2014,
Pubmed
Qu,
Functional geometry of the permeation pathway of Ca2+-activated Cl-channels inferred from analysis of voltage-dependent block.
2001,
Pubmed
,
Xenbase
Reinsprecht,
Blockade of capacitive Ca2+ influx by Cl- channel blockers inhibits secretion from rat mucosal-type mast cells.
1995,
Pubmed
Ryu,
Cloning and heterologous expression of new xANO2 from Xenopus laevis.
2011,
Pubmed
,
Xenbase
Schroeder,
Expression cloning of TMEM16A as a calcium-activated chloride channel subunit.
2008,
Pubmed
,
Xenbase
Seo,
Ani9, A Novel Potent Small-Molecule ANO1 Inhibitor with Negligible Effect on ANO2.
2016,
Pubmed
Ta,
Contrasting effects of phosphatidylinositol 4,5-bisphosphate on cloned TMEM16A and TMEM16B channels.
2017,
Pubmed
Takayama,
Modulation of water efflux through functional interaction between TRPV4 and TMEM16A/anoctamin 1.
2014,
Pubmed
Takayama,
Pain-enhancing mechanism through interaction between TRPV1 and anoctamin 1 in sensory neurons.
2015,
Pubmed
Thorneloe,
An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure.
2012,
Pubmed
Thorneloe,
N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I.
2008,
Pubmed
Toft-Bertelsen,
When size matters: transient receptor potential vanilloid 4 channel as a volume-sensor rather than an osmo-sensor.
2017,
Pubmed
,
Xenbase
Tong,
Calcium-Activated Chloride Channels in Newly Differentiating Mouse Lens Fiber Cells and Their Role in Volume Regulation.
2019,
Pubmed
Wang,
Overexpression of ANO1/TMEM16A, an arterial Ca2+-activated Cl- channel, contributes to spontaneous hypertension.
2015,
Pubmed
Wang,
Unexpected and differential effects of Cl- channel blockers on the Kv4.3 and Kv4.2 K+ channels. Implications for the study of the I(to2) current.
1997,
Pubmed
,
Xenbase
Wozniak,
The TMEM16A channel mediates the fast polyspermy block in Xenopus laevis.
2018,
Pubmed
,
Xenbase
Xiao,
Voltage- and calcium-dependent gating of TMEM16A/Ano1 chloride channels are physically coupled by the first intracellular loop.
2011,
Pubmed
Yang,
TMEM16A confers receptor-activated calcium-dependent chloride conductance.
2008,
Pubmed
,
Xenbase
Zeng,
TMEM16A regulates portal vein smooth muscle cell proliferation in portal hypertension.
2018,
Pubmed
Zhao,
TRP Channels Localize to Subdomains of the Apical Plasma Membrane in Human Fetal Retinal Pigment Epithelium.
2015,
Pubmed
