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Taxol Analogues Exhibit Differential Effects on Photoaffinity Labeling of β-Tubulin and the Multidrug Resistance

Chia-Ping Huang Yang1,2, Changwei Wang3, Iwao Ojima3

  • 1Department of Molecular Pharmacology , Albert Einstein College of Medicine , Bronx , New York 10461 , United States.

Journal of Natural Products
|March 9, 2018
PubMed

Insights

New taxanes, SB-T-1214 and SB-CST-10202, show potent activity against Taxol-resistant cancers by targeting βIII-tubulin and P-glycoprotein (P-gp). Their effectiveness varies based on drug resistance mechanisms in cancer cells.

Area of Science:

  • Pharmacology
  • Molecular Biology
  • Oncology

Background:

  • Taxol resistance in cancer is often mediated by βIII-tubulin overexpression and P-glycoprotein (P-gp) efflux.
  • Next-generation taxanes are being developed to overcome these resistance mechanisms.

Purpose of the Study:

  • To evaluate the distinct inhibitory effects of two novel taxanes, SB-T-1214 and SB-CST-10202, on β-tubulin and P-gp.
  • To assess the potency of these taxanes against various multidrug-resistant (MDR) cancer cell lines.

Main Methods:

  • Photoaffinity labeling with a Taxol analogue was used to study drug interactions with β-tubulin and P-gp.
  • Multidrug-resistant cell lines with varying levels of MDR1 and βIII-tubulin were generated and characterized.
  • Cytotoxicity assays were performed in the presence of verapamil to determine P-gp substrate activity.

Main Results:

  • SB-T-1214 and SB-CST-10202 demonstrated differential inhibition of β-tubulin photolabeling across eukaryotic sources.
  • Both taxanes inhibited P-gp photolabeling, correlating with [3H]vinblastine accumulation in MDR cells.
  • The taxanes exhibited distinct potencies against MSA-resistant cells with varying MDR1 and βIII-tubulin expression.
  • SB-T-1214 was identified as a P-gp substrate, though less so than Taxol.

Conclusions:

  • The effectiveness of novel taxanes is influenced by their interaction with multiple targets, including β-tubulin isotypes and P-gp.
  • SB-T-1214 and SB-CST-10202 represent promising candidates for treating cancers with specific drug resistance mechanisms.
  • Understanding the interplay between drug properties and cellular resistance factors is crucial for developing effective cancer therapies.

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