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Permanent link (DOI): https://doi.org/10.7939/R3Q815519

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Screening anti-cancer drugs against tubulin using catch-and-release electrospray ionization mass spectrometry Open Access

Descriptions

Author or creator
Darestani, Reza R.
Winter, Philip
Kitova, Elena N.
Tuszynski, Jack A.
Klassen, John S.
Additional contributors
Subject/Keyword
Tubulin
Binding
Drug
Affinity
Type of item
Journal Article (Published)
Language
English
Place
Time
Description
Tubulin, which is the building block of microtubules, plays an important role in cell division. This critical role makes tubulin an attractive target for the development of chemotherapeutic drugs to treat cancer. Currently, there is no general binding assay for tubulin–drug interactions. The present work describes the application of the catch-and-release electrospray ionization mass spectrometry (CaR-ESI-MS) assay to investigate the binding of colchicinoid drugs to αβ-tubulin dimers extracted from porcine brain. Proof-of-concept experiments using positive (ligands with known affinities) and negative (non-binders) controls were performed to establish the reliability of the assay. The assay was then used to screen a library of seven colchicinoid analogues to test their binding to tubulin and to rank their affinities.
Date created
2016
DOI
doi:10.7939/R3Q815519
License information
© 2016 Darestani, R. R., Winter, P., Kitova, E. N., Tuszynski, J. A., & Klassen, J. S. This version of this article is open access and can be downloaded and shared. The original author(s) and source must be cited.
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Citation for previous publication
Darestani, R. R., Winter, P., Kitova, E. N., Tuszynski, J. A., & Klassen, J. S. (2016). Screening anti-cancer drugs against tubulin using catch-and-release electrospray ionization mass spectrometry. Journal of the American Society for Mass Spectrometry, 27(5), 876-885.  http://doi.org/10.1007/s13361-016-1360-x

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