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Halogenation-Guided Chemical Screening Provides Insight into Tjipanazole Biosynthesis by the Cyanobacterium Fischerella ambigua.
ChemBioChem ( IF 3.2 ) Pub Date : 2020-03-17 , DOI: 10.1002/cbic.202000025
Tomasz Chilczuk 1 , Till F Schäberle 2, 3 , Sahel Vahdati 4 , Ute Mettal 2, 3 , Mustafa El Omari 5 , Heike Enke 6 , Michael Wiese 4 , Gabriele M König 5 , Timo H J Niedermeyer 1
Affiliation  

Seeking biosynthesis intermediates : The software tool HaloSeeker enabled us to detect halogenated tjipanazole derivatives in the complex HRMS data of an extract from the cyanobacterium F. ambigua . In conjunction with genomic data, this allowed us to propose a biosynthetic pathway for the tjipanazoles. Five isolated derivatives were tested for inhibition of the multidrug resistance transporter ABCG2, revealing structure‐activity relationships.
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中文翻译:

卤化引导的化学筛选提供了对蓝藻费氏菌生物合成替尼帕唑的深入了解。

寻找生物合成中间体:软件工具 HaloSeeker 使我们能够在蓝藻F. ambigua提取物的复杂 HRMS 数据中检测卤代吉帕唑衍生物。结合基因组数据,这使我们能够提出吉帕唑的生物合成途径。测试了五种分离的衍生物对多药耐药性转运蛋白 ABCG2 的抑制作用,揭示了结构-活性关系。
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更新日期:2020-03-17
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