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Mechanism of allosteric activation of TMEM16A/ANO1 channels by a commonly used chloride channel blocker

Abstract:

Calcium-activated chloride channels (CaCCs) play varied physiological roles and constitute potential therapeutic targets for conditions such as asthma and hypertension. TMEM16A encodes a CaCC. CaCC pharmacology is restricted to compounds with relatively low potency and poorly defined selectivity. Anthracene-9-carboxylic acid (A9C), an inhibitor of various chloride channel types, exhibits complex effects on native CaCCs and cloned TMEM16A channels providing both activation and inhibition. The ...

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Publication status:
Published
Peer review status:
Peer reviewed
Version:
Publisher's version

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Publisher copy:
10.1111/bph.13381

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Department:
Oxford, MSD, Pharmacology
Role:
Author
Wellcome Trust More from this funder
Biotechnology and Biological Sciences Research Council More from this funder
Publisher:
Wiley Online Library Publisher's website
Journal:
British Journal of Pharmacology Journal website
Volume:
173
Issue:
3
Pages:
511–528
Publication date:
2016-01-18
Acceptance date:
2015-11-12
DOI:
ISSN:
0007-1188 and 1476-5381
Pubs id:
pubs:598978
URN:
uri:feabe5d0-c909-416e-8002-7f8f8cd305b1
UUID:
uuid:feabe5d0-c909-416e-8002-7f8f8cd305b1
Local pid:
pubs:598978
Paper number:
3
Language:
English
Keywords:

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