Nature Communications (Jan 2020)

Elucidating target specificity of the taccalonolide covalent microtubule stabilizers employing a combinatorial chemical approach

  • Lin Du,
  • Samantha S. Yee,
  • Karthik Ramachandran,
  • April L. Risinger

DOI
https://doi.org/10.1038/s41467-019-14277-w
Journal volume & issue
Vol. 11, no. 1
pp. 1 – 13

Abstract

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Taccalonolide microtubule stabilizers covalently bind β-tubulin and overcome taxane resistance mechanisms. Here, the authors synthesized fluorogenic taccalonolide probes and investigated the specificity of taccalonolide binding to β-tubulin and the molecular interactions between drug and target,