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The TMEM16A blockers benzbromarone and MONNA cause intracellular Ca(2+)-release in mouse bronchial smooth muscle cells.
Dwivedi R, Drumm BT, Alkawadri T, Martin SL, Sergeant GP, Hollywood MA, Thornbury KD. Dwivedi R, et al. Eur J Pharmacol. 2023 May 15;947:175677. doi: 10.1016/j.ejphar.2023.175677. Epub 2023 Mar 24. Eur J Pharmacol. 2023. PMID: 36967079 Free article.
We investigated effects of TMEM16A blockers benzbromarone, MONNA, CaCC(inh)A01 and Ani9 on isometric contractions in mouse bronchial rings and on intracellular calcium in isolated bronchial myocytes. ...Iberiotoxin (0.3 muM) enhanced the contractions, but they were …
We investigated effects of TMEM16A blockers benzbromarone, MONNA, CaCC(inh)A01 and Ani9 on isometric contractions in mouse bro …
Asbestos Fibers Enhance the TMEM16A Channel Activity in Xenopus Oocytes.
Bernareggi A, Zangari M, Constanti A, Zacchi P, Borelli V, Mangogna A, Lorenzon P, Zabucchi G. Bernareggi A, et al. Membranes (Basel). 2023 Feb 1;13(2):180. doi: 10.3390/membranes13020180. Membranes (Basel). 2023. PMID: 36837683 Free PMC article.
RESULTS: The increase in chloride current after asbestos treatment, was sensitive to [Ca(2+)](e), and to specific blockers of TMEM16A Ca(2+)-activated chloride channels, MONNA and Ani9. Furthermore, asbestos treatment elevated the 'resting' [Ca(2+)](i) likelihood by …
RESULTS: The increase in chloride current after asbestos treatment, was sensitive to [Ca(2+)](e), and to specific blockers of TMEM16A …
Analysis of inhibitors of the anoctamin-1 chloride channel (transmembrane member 16A, TMEM16A) reveals indirect mechanisms involving alterations in calcium signalling.
Genovese M, Buccirossi M, Guidone D, De Cegli R, Sarnataro S, di Bernardo D, Galietta LJV. Genovese M, et al. Br J Pharmacol. 2023 Mar;180(6):775-785. doi: 10.1111/bph.15995. Epub 2022 Dec 18. Br J Pharmacol. 2023. PMID: 36444690 Free article.
We tested a panel of TMEM16A inhibitors, including CaCC(inh) -A01, niclosamide, MONNA, Ani9 and niflumic acid, to evaluate their possible effect on intracellular Ca(2+) . ...These effects were similarly observed in cells with and without TMEM16A expression. W …
We tested a panel of TMEM16A inhibitors, including CaCC(inh) -A01, niclosamide, MONNA, Ani9 and niflumic acid, to evaluate the …
TMEM16A (ANO1) as a therapeutic target in cystic fibrosis.
Galietta LJV. Galietta LJV. Curr Opin Pharmacol. 2022 Jun;64:102206. doi: 10.1016/j.coph.2022.102206. Epub 2022 Mar 29. Curr Opin Pharmacol. 2022. PMID: 35364521 Review.
Pharmacological stimulation of TMEM16A could be beneficial to bypass CFTR defect. However, the relationship of TMEM16A with mucus hypersecretion needs to be clarified. Multiple large scale screenings have been carried out to identify inhibitors and activators/potent …
Pharmacological stimulation of TMEM16A could be beneficial to bypass CFTR defect. However, the relationship of TMEM16A with mu …
Identification of evodiamine and rutecarpine as novel TMEM16A inhibitors and their inhibitory effects on peristalsis in isolated Guinea-pig ileum.
Zhao Z, Xue Y, Zhang G, Jia J, Xiu R, Jia Y, Wang Y, Wang X, Li H, Chen P, Zhang X. Zhao Z, et al. Eur J Pharmacol. 2021 Oct 5;908:174340. doi: 10.1016/j.ejphar.2021.174340. Epub 2021 Jul 12. Eur J Pharmacol. 2021. PMID: 34265294
The Lys(384), Thr(385), and Met(524) in TMEM16A are critical for evodiamine and rutecarpine's inhibitory effects. ...These findings demonstrate that evodiamine and rutecarpine are new TMEM16A inhibitors and support the regulation effect of TMEM16A modulators …
The Lys(384), Thr(385), and Met(524) in TMEM16A are critical for evodiamine and rutecarpine's inhibitory effects. ...These findings d …
Anoctamin 1 antagonism potentiates conventional tocolytic-mediated relaxation of pregnant human uterine smooth muscle.
Hyuga S, Parry RC, Danielsson J, Vink J, Fu XW, Wu A, Dan W, Yim PD, Gallos G. Hyuga S, et al. J Physiol Sci. 2021 Feb 22;71(1):7. doi: 10.1186/s12576-021-00792-3. J Physiol Sci. 2021. PMID: 33618673 Free PMC article.
In this study, we aimed to determine whether a combination of sub-relaxatory doses of tocolytic drugs in current clinical use [the L-type voltage-gated calcium channel (VGCC) blocker, nifedipine (NIF); and the beta(2)-adrenergic (beta2AR) agonist, terbutaline (TRB)] will potentia …
In this study, we aimed to determine whether a combination of sub-relaxatory doses of tocolytic drugs in current clinical use [the L-type vo …
Trophic sympathetic influence weakens pro-contractile role of Cl- channels in rat arteries during postnatal maturation.
Kostyunina DS, Zhang L, Shvetsova AA, Selivanova EK, Tarasova OS, Matchkov VV, Gaynullina DK. Kostyunina DS, et al. Sci Rep. 2020 Nov 17;10(1):20002. doi: 10.1038/s41598-020-77092-0. Sci Rep. 2020. PMID: 33203943 Free PMC article.
Cl(-) substitution in the solution as well as Cl(-)-channel blockers (MONNA, DIDS) had larger suppressive effect on the methoxamine-induced arterial contraction and methoxamine-induced depolarization of smooth muscle cells in 1- to 2-week-old compared to 2- to 3-month-old …
Cl(-) substitution in the solution as well as Cl(-)-channel blockers (MONNA, DIDS) had larger suppressive effect on the methoxamine-i …
TMEM16A is implicated in the regulation of coronary flow and is altered in hypertension.
Askew Page HR, Dalsgaard T, Baldwin SN, Jepps TA, Povstyan O, Olesen SP, Greenwood IA. Askew Page HR, et al. Br J Pharmacol. 2019 Jun;176(11):1635-1648. doi: 10.1111/bph.14598. Epub 2019 Apr 11. Br J Pharmacol. 2019. PMID: 30710335 Free PMC article.
Furthermore, we assessed whether any changes in expression and function occurred in coronary arteries from spontaneously hypertensive rats (SHRs). KEY RESULTS: TMEM16A was expressed in rat coronary arteries. The TMEM16A-specific inhibitor, MONNA, hyperpolaris …
Furthermore, we assessed whether any changes in expression and function occurred in coronary arteries from spontaneously hypertensive rats ( …
The TMEM16A channel mediates the fast polyspermy block in Xenopus laevis.
Wozniak KL, Phelps WA, Tembo M, Lee MT, Carlson AE. Wozniak KL, et al. J Gen Physiol. 2018 Sep 3;150(9):1249-1259. doi: 10.1085/jgp.201812071. Epub 2018 Jul 16. J Gen Physiol. 2018. PMID: 30012842 Free PMC article.
However, 2-(4-chloro-2-methylphenoxy)-N-[(2-methoxyphenyl)methylideneamino]-acetamide (Ani9) and N-((4-methoxy)-2-naphthyl)-5-nitroanthranilic acid (MONNA) each reduce xTMEM16A currents by more than 70% while only nominally inhibiting those generated by xBEST2A. Using whol …
However, 2-(4-chloro-2-methylphenoxy)-N-[(2-methoxyphenyl)methylideneamino]-acetamide (Ani9) and N-((4-methoxy)-2-naphthyl)-5-nitroanthranil …
Mechanisms of pruritogen-induced activation of itch nerves in isolated mouse skin.
Ru F, Sun H, Jurcakova D, Herbstsomer RA, Meixong J, Dong X, Undem BJ. Ru F, et al. J Physiol. 2017 Jun 1;595(11):3651-3666. doi: 10.1113/JP273795. Epub 2017 Mar 19. J Physiol. 2017. PMID: 28217875 Free PMC article.
Evidence is provided for a role for calcium-activated chloride channels such as TMEM16a in GPCR-activation of itch nerve terminals. The mechanism by which TRP channels participate in pruritogen-induced scratching may involve sites of action other than the primary afferent …
Evidence is provided for a role for calcium-activated chloride channels such as TMEM16a in GPCR-activation of itch nerve terminals. T …
11 results