التفاصيل البيبلوغرافية
| العنوان: |
Inhibition of ANO1/TMEM16A Chloride Channel by Idebenone and Its Cytotoxicity to Cancer Cell Lines. |
| المؤلفون: |
Seo, Yohan, Park, Jinhong, Kim, Minseo, Lee, Ho K., Kim, Jin-Hee, Jeong, Jin-Hyun, Namkung, Wan |
| المصدر: |
PLoS ONE; 7/21/2015, Vol. 10 Issue 7, p1-15, 15p |
| مصطلحات موضوعية: |
CHLORIDE channels, CELL-mediated cytotoxicity, CANCER cell culture, ENZYME inhibitors, CANCER cell proliferation, CYCLIC-AMP-dependent protein kinase |
| مستخلص: |
The expression levels of anoctamin 1 (ANO1, TMEM16A), a calcium-activated chloride channel (CaCC), are significantly increased in several tumors, and inhibition of ANO1 is known to reduce cell proliferation and migration. Here, we performed cell-based screening of a collection of natural products and drug-like compounds to identify inhibitors of ANO1. As a result of the screening, idebenone, miconazole and plumbagin were identified as novel ANO1 inhibitors. Electrophysiological studies showed that idebenone, a synthetic analog of coenzyme Q10, completely blocked ANO1 activity in FRT cells expressing ANO1 without any effect on intracellular calcium signaling and CFTR, a cAMP-regulated chloride channel. The CaCC activities in PC-3 and CFPAC-1 cells expressing abundant endogenous ANO1 were strongly blocked by idebenone. Idebenone inhibited cell proliferation and induced apoptosis in PC-3 and CFPAC-1 cells, but not in A549 cells, which do not express ANO1. These data suggest that idebenone, a novel ANO1 inhibitor, has potential for use in cancer therapy. [ABSTRACT FROM AUTHOR] |
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| قاعدة البيانات: |
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