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Channeling Relaxation through Multiple Means: TMEM16A Antagonism for Asthma.

作者信息

Jannu Arun K, Penn Raymond B

机构信息

Center for Translational Medicine Thomas Jefferson University Philadelphia, Pennsylvania.

出版信息

Am J Respir Cell Mol Biol. 2025 May;72(5):466-468. doi: 10.1165/rcmb.2024-0521ED.

DOI:10.1165/rcmb.2024-0521ED
PMID:39589219
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12051912/
Abstract
摘要
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2119/12051912/d3fa78249437/rcmb.2024-0521EDf1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2119/12051912/d3fa78249437/rcmb.2024-0521EDf1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2119/12051912/d3fa78249437/rcmb.2024-0521EDf1.jpg

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TMEM16A Antagonism: Therapeutic Potential with Desensitization of β-Agonist Responsiveness in Asthma.跨膜蛋白16A（TMEM16A）拮抗作用：对哮喘中β-激动剂反应性脱敏的治疗潜力
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Chloride ion transport and overexpression of TMEM16A in a guinea-pig asthma model.豚鼠哮喘模型中氯离子转运及TMEM16A的过表达
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本文引用的文献

1
TMEM16A Antagonism: Therapeutic Potential with Desensitization of β-Agonist Responsiveness in Asthma.跨膜蛋白16A（TMEM16A）拮抗作用：对哮喘中β-激动剂反应性脱敏的治疗潜力
Am J Respir Cell Mol Biol. 2025 May;72(5):510-519. doi: 10.1165/rcmb.2024-0231OC.
2
Identification of a β-arrestin-biased negative allosteric modulator for the β-adrenergic receptor.β-肾上腺素能受体的β-arrestin 偏向性负变构调节剂的鉴定。
Proc Natl Acad Sci U S A. 2023 Aug;120(31):e2302668120. doi: 10.1073/pnas.2302668120. Epub 2023 Jul 25.
3
In silico identification of a β-adrenoceptor allosteric site that selectively augments canonical βAR-Gs signaling and function.
通过计算机筛选出一种β-肾上腺素能受体变构位点，该位点选择性增强经典βAR-Gs 信号转导和功能。
Proc Natl Acad Sci U S A. 2022 Dec 6;119(49):e2214024119. doi: 10.1073/pnas.2214024119. Epub 2022 Nov 30.
4
The pharmacology of the TMEM16A channel: therapeutic opportunities.TMEM16A 通道的药理学：治疗机会。
Trends Pharmacol Sci. 2022 Sep;43(9):712-725. doi: 10.1016/j.tips.2022.06.006. Epub 2022 Jul 7.
5
Agonism of the TMEM16A calcium-activated chloride channel modulates airway smooth muscle tone.TMEM16A 钙激活氯离子通道激动剂调节气道平滑肌张力。
Am J Physiol Lung Cell Mol Physiol. 2020 Feb 1;318(2):L287-L295. doi: 10.1152/ajplung.00552.2018. Epub 2019 Nov 20.
6
Drug Repurposing: The Anthelmintics Niclosamide and Nitazoxanide Are Potent TMEM16A Antagonists That Fully Bronchodilate Airways.药物再利用：驱虫药氯硝柳胺和硝唑尼特是强效的TMEM16A拮抗剂，可使气道完全舒张。
Front Pharmacol. 2019 Feb 14;10:51. doi: 10.3389/fphar.2019.00051. eCollection 2019.
7
Activation mechanism of the calcium-activated chloride channel TMEM16A revealed by cryo-EM.冷冻电镜解析钙激活氯离子通道 TMEM16A 的激活机制。
Nature. 2017 Dec 21;552(7685):421-425. doi: 10.1038/nature24652. Epub 2017 Dec 13.
8
Structural basis for anion conduction in the calcium-activated chloride channel TMEM16A.钙激活氯离子通道TMEM16A中阴离子传导的结构基础。
Elife. 2017 May 31;6:e26232. doi: 10.7554/eLife.26232.
9
GPCRs and arrestins in airways: implications for asthma.气道中的G蛋白偶联受体与抑制蛋白：对哮喘的影响
Handb Exp Pharmacol. 2014;219:387-403. doi: 10.1007/978-3-642-41199-1_20.
10
Calcium-activated chloride channel TMEM16A modulates mucin secretion and airway smooth muscle contraction.钙激活氯离子通道 TMEM16A 调节粘蛋白分泌和气道平滑肌收缩。
Proc Natl Acad Sci U S A. 2012 Oct 2;109(40):16354-9. doi: 10.1073/pnas.1214596109. Epub 2012 Sep 17.