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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
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container_title Angewandte Chemie (International ed.)
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creator Kumar, Ashutosh
Heise, Henrike
Blommers, Marcel J.J
Krastel, Philipp
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Mandelkow, Eva-Maria
Carlomagno, Teresa
Griesinger, Christian
Baldus, Marc
description 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)).
doi_str_mv 10.1002/anie.201001946
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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
title Interaction of Epothilone B (Patupilone) with Microtubules as Detected by Two-Dimensional Solid-State NMR Spectroscopy
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