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Molecular basis for inhibition of AcrB multidrug efflux pump by novel and powerful pyranopyridine derivatives [Biochemistry]
Proceedings of the National Academy of Sciences of the United States of America ( IF 9.4 ) Pub Date : 2016-03-29 09:15:46 , DOI: 10.1073/pnas.1602472113
Hanno Sjuts 1 , Attilio V. Vargiu 2 , Steven M. Kwasny 3 , Son T. Nguyen 3 , Hong-Suk Kim 4 , Xiaoyuan Ding 3 , Alina R. Ornik 1 , Paolo Ruggerone 2 , Terry L. Bowlin 3 , Hiroshi Nikaido 4 , Klaas M. Pos 1 , Timothy J. Opperman 3
Affiliation  

The Escherichia coli AcrAB-TolC efflux pump is the archetype of the resistance nodulation cell division (RND) exporters from Gram-negative bacteria. Overexpression of RND-type efflux pumps is a major factor in multidrug resistance (MDR), which makes these pumps important antibacterial drug discovery targets. We have recently developed novel pyranopyridine-based inhibitors of...

中文翻译:

新型强力吡喃吡啶衍生物抑制AcrB多药外排泵的分子基础[生物化学]

大肠杆菌AcrAB-TolC外排泵是革兰氏阴性细菌耐药结节性细胞分裂(RND)出口者的原型。RND型外排泵的过表达是多药耐药性(MDR)的主要因素,这使这些泵成为重要的抗菌药物发现目标。我们最近开发了新型的以吡喃吡啶为基础的抑制剂...
更新日期:2016-04-01
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