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

  • Author(s) / Creator(s)
  • 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
  • Subjects / Keywords
  • Type of Item
    Article (Published)
  • DOI
    https://doi.org/10.7939/R3Q815519
  • License
    © 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
  • Link to related item
    http://doi.org/10.1007/s13361-016-1360-x