A fluorescence anisotropy assay to discover and characterize ligands targeting the maytansine site of tubulin

Grégory Menchon; Andrea E. Prota; Daniel Lucena-Agell; Pascal Bucher; Rolf Jansen; Herbert Irschik; Rolf Müller; Ian Paterson; J. Fernando Díaz; Karl-Heinz Altmann; Michel O. Steinmetz

doi:10.1038/s41467-018-04535-8

Nature Communications (May 2018)

A fluorescence anisotropy assay to discover and characterize ligands targeting the maytansine site of tubulin

Grégory Menchon,
Andrea E. Prota,
Daniel Lucena-Agell,
Pascal Bucher,
Rolf Jansen,
Herbert Irschik,
Rolf Müller,
Ian Paterson,
J. Fernando Díaz,
Karl-Heinz Altmann,
Michel O. Steinmetz

Affiliations

Grégory Menchon: Laboratory of Biomolecular Research, Division of Biology and Chemistry, Paul Scherrer Institut
Andrea E. Prota: Laboratory of Biomolecular Research, Division of Biology and Chemistry, Paul Scherrer Institut
Daniel Lucena-Agell: Chemical and Physical Biology, Centro de Investigaciones Biológicas, Consejo Superior de Investigaciones Cientificas CIB–CSIC
Pascal Bucher: Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, ETH Zürich
Rolf Jansen: Abteilung Mikrobielle Wirkstoffe, Helmholtz Zentrum für Infektionsforschung
Herbert Irschik: Abteilung Mikrobielle Wirkstoffe, Helmholtz Zentrum für Infektionsforschung
Rolf Müller: Department Microbial Natural Products and Department of Pharmacy at Saarland University, Helmholtz Institute for Pharmaceutical Research Saarland, Helmholtz Centre for Infection Research
Ian Paterson: University Chemical Laboratory, Cambridge University
J. Fernando Díaz: Chemical and Physical Biology, Centro de Investigaciones Biológicas, Consejo Superior de Investigaciones Cientificas CIB–CSIC
Karl-Heinz Altmann: Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, ETH Zürich
Michel O. Steinmetz: Laboratory of Biomolecular Research, Division of Biology and Chemistry, Paul Scherrer Institut

DOI: https://doi.org/10.1038/s41467-018-04535-8
Journal volume & issue: Vol. 9, no. 1
pp. 1 – 9

Abstract

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Microtubule-targeting agents are used successfully as anticancer therapeutics. Here authors develop a fluorescence-anisotropy-based assay to identify and characterize ligands for the maytansine site of tubulin and provide crystal structures of identified ligands in complex with tubulin.

Published in Nature Communications

ISSN: 2041-1723 (Online)
Publisher: Nature Portfolio
Country of publisher: United Kingdom
LCC subjects: Science
Website: https://www.nature.com/ncomms/

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