Interaction of Epothilone B (Patupilone) with Microtubules as Detected by Two-Dimensional Solid-State NMR Spectroscopy

Solid evidence: Induction of the polymerization of αβ‐tubulin dimers into microtubules by epothilones, such as patupilone, by an as yet unknown mechanism leads to the apoptosis of cancer cells. Solid‐state NMR spectroscopy of patupilone bound to microtubules has now enabled the identification of ato...

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Published in:Angewandte Chemie (International ed.) 2010-10, Vol.49 (41), p.7504-7507
Main Authors: Kumar, Ashutosh, Heise, Henrike, Blommers, Marcel J.J, Krastel, Philipp, Schmitt, Esther, Petersen, Frank, Jeganathan, Siva, Mandelkow, Eva-Maria, Carlomagno, Teresa, Griesinger, Christian, Baldus, Marc
Format: Article
Language:English
Subjects:
Antineoplastic Agents - isolation & purification
Antineoplastic Agents - pharmacology
antitumor agents
drug binding
Epothilones - isolation & purification
Epothilones - pharmacology
Humans
microtubules
Microtubules - metabolism
Microtubules - ultrastructure
Models, Molecular
Myxococcales - chemistry
Neoplasms - drug therapy
NMR spectroscopy
Nuclear Magnetic Resonance, Biomolecular - methods
structure elucidation
Tubulin - metabolism
Tubulin Modulators - isolation & purification
Tubulin Modulators - pharmacology
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Summary:Solid evidence: Induction of the polymerization of αβ‐tubulin dimers into microtubules by epothilones, such as patupilone, by an as yet unknown mechanism leads to the apoptosis of cancer cells. Solid‐state NMR spectroscopy of patupilone bound to microtubules has now enabled the identification of atomic positions of the drug that undergo clear chemical‐shift changes upon binding (see correlation spectra of free (black) and complexed patupilone (red)).
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.201001946