The high-resolution solution structure of epothilone A bound to tubulin: An understanding of the structure-activity relationships for a powerful class of antitumor agents

被引：87

作者：

Carlomagno, T

Blommers, MJJ

Meiler, J

Jahnke, W

Schupp, T

Petersen, F

Schinzer, D

Altmann, KH

Griesinger, C

机构：

[1] Max Planck Inst Biophys Chem, D-37077 Gottingen, Germany

[2] Novartis Pharma AG, Core Technol, CH-4002 Basel, Switzerland

[3] Novartis Pharma AG, Lead Discovery Ctr, CH-4002 Basel, Switzerland

[4] Novartis Pharma AG, Corp Res, CH-4002 Basel, Switzerland

[5] Univ Magdeburg, Inst Chem, D-39106 Magdeburg, Germany

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2003年 / 42卷 / 22期

关键词：

natural products; NMR spectroscopy; structure elucidation; structure-activity relationships; tubulin;

D O I：

10.1002/anie.200351276

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The tubulin-bound structure of epothilone A (shown in green) differs substantially from its free conformation (determined by X-ray crystallography, shown in gray). The new structural data correlate well with results from chemical modification experiments, giving a consistent picture of the functionally important regions of epothilone.

引用

页码：2511 / 2515

页数：5

共 44 条

[11] Stabilization of tubulin by deuterium oxide [J].