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对四环素抗性外排泵具有选择性作用的化合物。

Compounds that select against the tetracycline-resistance efflux pump.

作者信息

Stone Laura K, Baym Michael, Lieberman Tami D, Chait Remy, Clardy Jon, Kishony Roy

机构信息

Department of Systems Biology, Harvard Medical School, Boston, Massachusetts, USA.

Institute of Science and Technology-Austria, Maria Gugging 3400, Klosterneuburg, Austria.

出版信息

Nat Chem Biol. 2016 Nov;12(11):902-904. doi: 10.1038/nchembio.2176. Epub 2016 Sep 19.

DOI:10.1038/nchembio.2176
PMID:27642863
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5069154/
Abstract

We developed a competition-based screening strategy to identify compounds that invert the selective advantage of antibiotic resistance. Using our assay, we screened over 19,000 compounds for the ability to select against the TetA tetracycline-resistance efflux pump in Escherichia coli and identified two hits, β-thujaplicin and disulfiram. Treating a tetracycline-resistant population with β-thujaplicin selects for loss of the resistance gene, enabling an effective second-phase treatment with doxycycline.

摘要

我们开发了一种基于竞争的筛选策略，以鉴定能够逆转抗生素耐药性选择优势的化合物。利用我们的检测方法，我们筛选了超过19000种化合物，以检测其针对大肠杆菌中TetA四环素耐药性外排泵的选择能力，并鉴定出两种有效化合物，即β-崖柏素和双硫仑。用β-崖柏素处理四环素耐药群体可导致耐药基因丢失，从而能够用强力霉素进行有效的第二阶段治疗。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0606/5069154/36b37a5066e8/nihms803517f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0606/5069154/66f169a1b899/nihms803517f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0606/5069154/36b37a5066e8/nihms803517f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0606/5069154/66f169a1b899/nihms803517f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0606/5069154/36b37a5066e8/nihms803517f2.jpg

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