Article (Scientific journals)
Microtubule targeting agents: from biophysics to proteomics
Calligaris, David; Verdier-Pinard, Pascal; Devred, François et al.
2010In Cellular and Molecular Life Sciences, 67 (7), p. 1089-1104
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Abstract :
[en] This review explores various aspects of the interaction between microtubule targeting agents and tubulin, including binding site, affinity, and drug resistance. Starting with the basics of tubulin polymerization and microtubule targeting agent binding, we then highlight how the three-dimensional structures of drug-tubulin complexes obtained on stabilized tubulin are seeded by precise biological and biophysical data. New avenues opened by thermodynamics analysis, high throughput screening, and proteomics for the molecular pharmacology of these drugs are presented. The amount of data generated by biophysical, proteomic and cellular techniques shed more light onto the microtubule-tubulin equilibrium and tubulin-drug interaction. Combining these approaches provides new insight into the mechanism of action of known microtubule interacting agents and rapid in-depth characterization of next generation molecules targeting the interaction between microtubules and associated modulators of their dynamics. This will facilitate the design of improved and/or alternative chemotherapies targeting the microtubule cytoskeleton.
Disciplines :
Oncology
Author, co-author :
Calligaris, David ;  Université de Liège - ULiège > Département de chimie (sciences) > GIGA-R : Laboratoire de spectrométrie de masse (L.S.M.)
Verdier-Pinard, Pascal
Devred, François
Villard, Claude
Braguer, Diane
Lafitte, Daniel
Language :
English
Title :
Microtubule targeting agents: from biophysics to proteomics
Publication date :
April 2010
Journal title :
Cellular and Molecular Life Sciences
ISSN :
1420-682X
eISSN :
1420-9071
Publisher :
Birkhäuser, Basel, Switzerland
Volume :
67
Issue :
7
Pages :
1089-1104
Peer reviewed :
Peer Reviewed verified by ORBi
Available on ORBi :
since 04 July 2012

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