Isolation of proflavine as a blocker of G protein-gated inward rectifier potassium channels by a cell growth-based screening system
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- 作者：Hitoshi Kawadaa ; Atsushi Inanobea ; b ; inanobe@pharma2.med.osaka-u.ac.jp" class="auth_mail" title="E-mail the corresponding author ; Yoshihisa Kurachia ; b ; ykurachi@pharma2.med.osaka-u.ac.jp" class="auth_mail" title="E-mail the corresponding author
- 关键词：G protein-gated inward rectifier K+ channels ; Drug screening ; Proflavine ; Channel blocker
- 刊名：Neuropharmacology
- 出版年：2016
- 出版时间：October 2016
- 年：2016
- 卷：109
- 期：Complete
- 页码：18-28
- 全文大小：1390 K
文摘
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Compounds that block Kir3.2 are expected to improve the symptoms of Down syndrome.
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A K+ transporter-deficient yeast strain was used for screening Kir3.2 blockers.
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Proflavine was isolated to inhibit the growth of Kir3.2-transformant cells.
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Proflavine behaves as a pore blocker for Kir3.2.
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Proflavine is a potential lead compound for Kir3.2-associated neurological diseases.