Screening Anti-Cancer Drugs against Tubulin using Catch-and-Release Electrospray Ionization Mass Spectrometry

2016/03/04 by Reza Rezaei Darestani, Philip Winter, Elena N. Kitova +3
Chemistry · Medicine · #Analytical Chemistry and Chromatography #Cancer Treatment and Pharmacology #Mass Spectrometry Techniques and Applications

paper · doi:10.1007/s13361-016-1360-x

openalex publication_date 2016/03/04 · openalex created_date 2025/10/10 · openalex updated_date 2026/07/23

Abstract

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.

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