A Substrate Mimic Allows High-Throughput Assay of the FabA Protein and Consequently the Identification of a Novel Inhibitor of Pseudomonas aeruginosa FabA
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- 作者：Lucile Moynié ; 1 ; lm108@st-andrews.ac.uk" class="auth_mail" title="E-mail the corresponding author ; Anthony G. Hope2 ; a.g.hope@dundee.ac.uk" class="auth_mail" title="E-mail the corresponding author ; Kara Finzel3 ; kfinzel@ucsd.edu" class="auth_mail" title="E-mail the corresponding author ; Jason Schmidberger4 ; jason.schmidberger@gmail.com" class="auth_mail" title="E-mail the corresponding author ; Stuart M. Leckie1 ; leckiestm@gmail.com" class="auth_mail" title="E-mail the corresponding author ; Gunter Schneider4 ; Gunter.Schneider@ki.se" class="auth_mail" title="E-mail the corresponding author ; Michael D. Burkart3 ; mburkart@ucsd.edu" class="auth_mail" title="E-mail the corresponding author ; Andrew D. Smith1 ; ads10@st-andrews.ac.uk" class="auth_mail" title="E-mail the corresponding author ; David W. Gray2 ; d.w.gray@dundee.ac.uk" class="auth_mail" title="E-mail the corresponding author ; James H. Naismith1 ; 5 ; naismith@st-andrew.ac.uk" class="auth_mail" title="E-mail the corresponding author
- 关键词：ACP ; acyl carrier protein ; NAC ; N-acetylcysteamine ; N42FTA ; N-(4-chlorobenzyl)-3-(2-furyl)-1H-1 ; 2 ; 4-triazol-5-amine ; FAS ; fatty acid synthase ; TEV ; tobacco etch virus
- 刊名：Journal of Molecular Biology
- 出版年：2016
- 出版时间：16 January 2016
- 年：2016
- 卷：428
- 期：1
- 页码：108-120
- 全文大小：1575 K
文摘
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FabA is a promising drug target in Gram-negative bacteria.
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High-throughput coupled assay for FabA using a substrate analogue has been developed.
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New class of non-covalent inhibitor has been identified using the assay.
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The compound inhibits the biological activity of FabA.
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Crystal structure of the compound bound to FabA has been determined.