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前微管溶素,一种来自盘状血管球菌的强效且化学性质可及的微管溶素前体。

Pretubulysin, a potent and chemically accessible tubulysin precursor from Angiococcus disciformis.

作者信息

Ullrich Angelika, Chai Yi, Pistorius Dominik, Elnakady Yasser A, Herrmann Jennifer E, Weissman Kira J, Kazmaier Uli, Müller Rolf

机构信息

Institut für Organische Chemie, Universität des Saarlandes, Postfach 151150, 66041 Saarbrücken, Germany.

出版信息

Angew Chem Int Ed Engl. 2009;48(24):4422-5. doi: 10.1002/anie.200900406.

Abstract

Simplify, simplify, simplify! Pretubulysin (structure without the green substituents), a simplified tubulysin was prepared in the laboratory and also found in a natural myxobacterial source. This biosynthetic precursor of the tubulysins is not as active as tubulysins A and D but is still effective in picomolar concentrations against cancer cell lines.

摘要

简化,简化,再简化!前微管溶素(无绿色取代基的结构),一种简化的微管溶素,已在实验室制备出来,并且也在一种天然粘细菌来源中被发现。微管溶素的这种生物合成前体不如微管溶素A和D那样具有活性,但在皮摩尔浓度下对癌细胞系仍有效果。

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