Abstract

The development of resistance to paclitaxel in tumors is one of the most significant obstacles to successful therapy. Overexpression of the betaIII-tubulin isotype has been associated with paclitaxel resistance in a number of cancer cell lines and in tumors, but the mechanism of resistance has remained unclear. Paclitaxel inhibits cancer cell proliferation by binding to the beta-subunit of tubulin in microtubules and suppressing microtubule dynamic instability, leading to mitotic arrest and cell death. We hypothesized that betaIII-tubulin overexpression induces resistance to paclitaxel either by constitutively enhancing microtubule dynamic instability in resistant cells or by rendering the microtubules less sensitive to the suppression of dynamics by paclitaxel. Using Chinese hamster ovary cells that inducibly overexpress either betaI- or betaIII-tubulin, we analyzed microtubule dynamic instability during interphase by microinjection of rhodamine-labeled tubulin and time-lapse fluorescence microscopy. In the absence of paclitaxel, there were no differences in any aspect of dynamic instability between the two beta-tubulin-overexpressing cell types. However, in the presence of 150 nm paclitaxel, dynamic instability was suppressed to a significantly lesser extent (suppressed only 12%) in cells overexpressing betaIII-tubulin than in cells overexpressing similar levels of betaI-tubulin (suppressed 47%). The results suggest that overexpression of betaIII-tubulin induces paclitaxel resistance by reducing the ability of paclitaxel to suppress microtubule dynamics. The results also suggest that endogenous regulators of microtubule dynamics may differentially interact with individual tubulin isotypes, supporting the idea that differential expression of tubulin isotypes has functional consequences in cells.

Highlights

  • The development of resistance to paclitaxel in tumors is one of the most significant obstacles to successful therapy

  • We found that ␤III-tubulin overexpression induces paclitaxel resistance by decreasing the efficacy of paclitaxel binding to ␤III-tubulin, resulting in a weaker suppressive effect on microtubule dynamics

  • The results are the first direct demonstration that drugs can differentially interact with different tubulin isotypes in cells, suggesting that microtubule dynamic instability might be regulated by the differential interaction of endogenous regulators with the individual isotypes as well

Read more

Summary

Introduction

The development of resistance to paclitaxel in tumors is one of the most significant obstacles to successful therapy. Paclitaxel inhibits cancer cell proliferation by binding to the ␤-subunit of tubulin in microtubules and suppressing microtubule dynamic instability, leading to mitotic arrest and cell death. We hypothesized that ␤III-tubulin overexpression induces resistance to paclitaxel either by constitutively enhancing microtubule dynamic instability in resistant cells or by rendering the microtubules less sensitive to the suppression of dynamics by paclitaxel. The results suggest that overexpression of ␤III-tubulin induces paclitaxel resistance by reducing the ability of paclitaxel to suppress microtubule dynamics. Because the lowest concentrations of paclitaxel that effectively inhibit cell proliferation and block mitosis suppress microtubule dynamics [6, 12, 13] without significantly increasing microtubule polymer levels, suppression of microtubule dynamics appears to be its most potent mechanism of mitotic arrest [14]. The functional significance of variations in tubulin isotype expression in both normal and tumor cells is not known

Methods
Results
Conclusion
Full Text
Published version (Free)

Talk to us

Join us for a 30 min session where you can share your feedback and ask us any queries you have

Schedule a call