Protein-degrading enediynes: library screening of Bergman cycloaromatization products.
Protein-degrading enediynes: library screening of Bergman cycloaromatization products.
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蛋白质降解烯二炔：伯格曼环芳构化产物的文库筛选。
DOI：
10.1021/ol005926q
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发表时间：
2000
期刊：
影响因子：
5.2
通讯作者：
Brown,MA
中科院分区：
文献类型：
--
作者：
Jones,GB;Wright,JM;Hynd,G;Wyatt,JK;Yancisin,M;Brown,MA
基于伯格曼环芳构化产物的筛选方法应用于雌激素-烯二炔杂合体的紧凑文库。随后合成了从筛选中鉴定出的候选烯二炔，它在环芳构化后诱导人雌激素受体α发生温度和浓度依赖性降解。
A screening method based on Bergman cycloaromatization products was applied to a compact library of estrogenic-enediyne hybrids. An enediyne candidate identified from the screen was subsequently synthesized, and it induced temperature- and concentration-dependent degradation of human estrogen receptor α upon cycloaromatization.