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用于鉴定膜结合能量转换蛋白抑制剂的脂质和去污剂酶环境比较

Comparison of lipid and detergent enzyme environments for identifying inhibitors of membrane-bound energy-transducing proteins.

作者信息

Dunn Elyse A, Cook Gregory M, Heikal Adam

机构信息

Department of Microbiology and Immunology, University of Otago, Dunedin 9054, New Zealand.

Department of Microbiology and Immunology, University of Otago, Dunedin 9054, New Zealand; Maurice Wilkins Centre for Molecular Biodiscovery, The University of Auckland, Private Bag 92019, Auckland 1042, New Zealand.

出版信息

J Microbiol Methods. 2016 Jan;120:41-3. doi: 10.1016/j.mimet.2015.11.012. Epub 2015 Nov 28.

DOI:10.1016/j.mimet.2015.11.012
PMID:26593449
Abstract

This study compared detergent-solubilised (soluble) and lipid-reconstituted (proteoliposome) protein to establish a high-throughput method for identifying membrane protein inhibitors. We identified inhibitors of the membrane-bound type II NADH dehydrogenase with lower lipophilicity and better potency, suggesting proteoliposome systems may be advantageous over detergent-solubilised systems for respiratory membrane proteins.

摘要

本研究比较了去污剂增溶(可溶性)蛋白和脂质重构(蛋白脂质体)蛋白,以建立一种高通量方法来鉴定膜蛋白抑制剂。我们鉴定出了亲脂性较低且效力更佳的膜结合型II NADH脱氢酶抑制剂,这表明对于呼吸膜蛋白而言,蛋白脂质体系统可能比去污剂增溶系统更具优势。

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Annotated compound data for modulators of detergent-solubilised or lipid-reconstituted respiratory type II NADH dehydrogenase activity obtained by compound library screening.通过化合物库筛选获得的用于去污剂增溶或脂质重构的呼吸性II型NADH脱氢酶活性调节剂的注释化合物数据。
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