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Combinatorial Strategies and High Throughput Screening in Drug Discovery Targeted to the Channel of Botulinum Neurotoxin

机译：药物发现中的组合策略和高通量筛选针对肉毒杆菌神经毒素通道

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The ultimate goal of this program is to discover selective and potent drugs targeted to prevent or relieve the neurotoxic actions of botulinum neurotoxin (BoNT) A. A major goal of this program is the identification of open channel blockers as a single class of drugs that would be effective against all BoNT isoforms. We consider the BoNT channel as a validated target for intervention aimed to inhibit the translocation of the light chain into the cytosol and therefore to attenuate the BoNT neurotoxicity. The major focus thus far has been the implementation of a reliable and robust high-throughput screen for blockers specific for BoNT using Neuro 2A cells in which BoNTA forms channels with similar properties to those previously characterized in lipid bilayers. The immediate task during the present reporting period involved the detailed characterization of the channel and chaperone activity of BoNTA on Neuro2A cells.

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作者
Montal, M.;
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年度 2006
页码 1-16
总页数 16
原文格式 PDF
正文语种 eng
中图分类工业技术;
关键词
Clostridium botulinum; Neurotoxins; High rate; Strategy; Validation; Layers; Lipids; Targets; Medical screening; Translocation; Throughput; Lightweight; Combinatorial analysis; Drugs; Potency; Bacterial toxins;

机译：肉毒杆菌;神经毒素;高比率;策略;验证;层;脂质;目标;医学筛查;易位;吞吐量;轻量;组合分析;药物;效力;细菌毒素;

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2. Embryonic stem cell-derived motoneurons provide a highly sensitive cell culture model for botulinum neurotoxin studies, with implications for high-throughput drug discovery - ScienceDirect [J] . Erkan Kiris, Jonathan E. Nuss, James C. Burnett, Stem cell research . 2011,第3期

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6. Embryonic stem cell derived motoneurons provide a highly sensitive cell culture model for botulinum neurotoxin studies with implications for high-throughput drug discovery [O] . Erkan Kiris, Jonathan E. Nuss, James C. Burnett, -1

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7. Embryonic stem cell-derived motoneurons provide a highly sensitive cell culture model for botulinum neurotoxin studies, with implications for high-throughput drug discovery [O] . Kiris Erkan, Nuss Jonathan E., Burnett James C., 2011

机译：胚胎干细胞衍生的运动神经元为肉毒杆菌神经毒素研究提供了高度敏感的细胞培养模型，对高通量药物发现具有重要意义

Combinatorial Strategies and High Throughput Screening in Drug Discovery Targeted to the Channel of Botulinum Neurotoxin

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