Much Anticipated—The Bioactive Conformation of Epothilone and Its Binding to Tubulin
Dirk W. Heinz, Wolf‐Dieter Schubert, Gerhard Höfle
Abstract
Dirk W. Heinz, Wolf‐Dieter Schubert, Gerhard Höfle
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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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