2005Angewandte Chemie International EditionRequires access

Much Anticipated—The Bioactive Conformation of Epothilone and Its Binding to Tubulin

Dirk W. Heinz, Wolf‐Dieter Schubert, Gerhard Höfle

Open publisher page 56 citations

Abstract

Filled pockets: Epothilones initiate apoptosis in eukaryotic cells by inducing extensive polymerization of αβ-tubulin. Until recently, little was known about the binding mode of epothilones within the tubulin binding cavity. The structure of the epothilone A/tubulin complex (see picture) determined by electron crystallography has dramatically reversed the situation.

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What this paper is about

Filled pockets: Epothilones initiate apoptosis in eukaryotic cells by inducing extensive polymerization of αβ-tubulin. Until recently, little was known about the binding mode of epothilones within the tubulin binding cavity. The structure of the epothilone A/tubulin complex (see picture) determined by electron crystallography has dramatically reversed the situation.

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Available abstract

Filled pockets: Epothilones initiate apoptosis in eukaryotic cells by inducing extensive polymerization of αβ-tubulin. Until recently, little was known about the binding mode of epothilones within the tubulin binding cavity. The structure of the epothilone A/tubulin complex (see picture) determined by electron crystallography has dramatically reversed the situation.

Key concepts: Epothilones, Epothilone, Tubulin, Microtubule, Chemistry, Stereochemistry, Cell biology, Biophysics

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