Direkt zum Inhalt

Kunzelmann, Karl ; Centeio, Raquel ; Ousingsawat, Jiraporn ; Cabrita, Inês ; Schreiber, Rainer ; Talbi, Khaoula ; Benedetto, Roberta ; Doušová, Tereza ; Verbeken, Eric K. ; De Boeck, Kris ; Cohen, Isaac

Mucus Release and Airway Constriction by TMEM16A May Worsen Pathology in Inflammatory Lung Disease

Article

Kunzelmann, Karl , Centeio, Raquel, Ousingsawat, Jiraporn , Cabrita, Inês , Schreiber, Rainer , Talbi, Khaoula, Benedetto, Roberta, Doušová, Tereza , Verbeken, Eric K., De Boeck, Kris and Cohen, Isaac (2021) Mucus Release and Airway Constriction by TMEM16A May Worsen Pathology in Inflammatory Lung Disease. International Journal of Molecular Sciences 22 (7852), pp. 1-18.

DOI to cite this document: 10.5283/epub.46060


Abstract

Activation of the Ca2+ activated Cl- channel TMEM16A is proposed as a treatment in inflammatory airway disease. It is assumed that activation of TMEM16A will induce electrolyte secretion, and thus reduce airway mucus plugging and improve mucociliary clearance. A benefit of activation of TMEM16A was shown in vitro and in studies in sheep, but others reported an increase in mucus production and ...

Activation of the Ca2+ activated Cl- channel TMEM16A is proposed as a treatment in inflammatory airway disease. It is assumed that activation of TMEM16A will induce electrolyte secretion, and thus reduce airway mucus plugging and improve mucociliary clearance. A benefit of activation of TMEM16A was shown in vitro and in studies in sheep, but others reported an increase in mucus production and airway contraction by activation of TMEM16A. We analyzed expression of TMEM16A in healthy and inflamed human and mouse airways and examined the consequences of activation or inhibition of TMEM16A in asthmatic mice. TMEM16A was found to be upregulated in the lungs of patients with asthma or cystic fibrosis, as well as in the airways of asthmatic mice. Activation or potentiation of TMEM16A by the compounds Eact or brevenal, respectively, induced acute mucus release from airway goblet cells and induced bronchoconstriction in mice in vivo. In contrast, niclosamide, an inhibitor of TMEM16A, blocked mucus production and mucus secretion in vivo and in vitro. Treatment of airway epithelial cells with niclosamide strongly inhibited expression of the essential transcription factor of Th2-dependent inflammation and goblet cell differentiation, SAM pointed domain-containing ETS-like factor (SPDEF). Activation of TMEM16A in people with inflammatory airway diseases is likely to induce mucus secretion along with airway constriction. In contrast, inhibitors of TMEM16A may suppress pulmonary Th2 inflammation, goblet cell metaplasia, mucus production, and bronchoconstriction, partially by inhibiting expression of SPDEF.



Involved Institutions


Details

Item typeArticle
Journal or Publication TitleInternational Journal of Molecular Sciences
PublisherMDPI
Open Access TypeGold (with APC)
Place of PublicationBASEL
Volume22
Number of Issue or Book Chapter7852
Page Rangepp. 1-18
Date21 July 2021
Date of publication25 Jan 2022 15:14
InstitutionsBiology, Preclinical Medicine > Institut für Physiologie > Prof. Dr. Karl Kunzelmann
Identification Number
ValueType
10.3390/ijms22157852DOI
KeywordsACTIVATED CHLORIDE CHANNEL; CA2+-ACTIVATED CL-CHANNEL; CYSTIC-FIBROSIS; SMOOTH-MUSCLE; MUCOCILIARY CLEARANCE; SECRETION; MUCIN; ASTHMA; HYPERRESPONSIVENESS; OVEREXPRESSION; TMEM16A; ETX001; Eact; brevenal; asthma; cystic fibrosis; airways
Dewey Decimal Classification500 Science > 570 Life sciences
StatusPublished
RefereedYes, this version has been refereed
Created at the University of RegensburgYes
URN of the UB Regensburgurn:nbn:de:bvb:355-epub-460605
Item ID46060

Export bibliographical data

Owner only: item control page

nach oben