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

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dc.contributor.authorKitova, Elena N.
dc.contributor.authorKlassen, John S.
dc.contributor.authorWinter, Philip
dc.contributor.authorTuszynski, Jack A.
dc.contributor.authorDarestani, Reza R.
dc.date.accessioned2025-05-01T12:11:36Z
dc.date.available2025-05-01T12:11:36Z
dc.date.issued2016
dc.descriptionTubulin, 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.
dc.identifier.doihttps://doi.org/10.7939/R3Q815519
dc.language.isoen
dc.relationhttp://doi.org/10.1007/s13361-016-1360-x
dc.relation.isversionofDarestani, 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
dc.rights© 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.
dc.subjectTubulin
dc.subjectBinding
dc.subjectAffinity
dc.subjectDrug
dc.titleScreening anti-cancer drugs against tubulin using catch-and-release electrospray ionization mass spectrometry
dc.typehttp://purl.org/coar/resource_type/c_6501 http://purl.org/coar/version/c_970fb48d4fbd8a85
ual.jupiterAccesshttp://terms.library.ualberta.ca/public

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