Microtubule-targeting agents(MTAs)such as paclitaxel and the vincaalkaloids are among the most important medical weapons available to combat cancer. MTAs interfere with intracellular transport, inhibit eukaryotic cell proliferation, and promote cell death by suppressing microtubule dynamics. Recent advan-ces in the structural analysis of MTAs have enabled the extensive characterization of their interactions with microtubules and their building block tubulin. We revie where our current knowledge on the molecular mechanisms used by MTAs to hijack the microtubule cytoskeleton,and discuss dual inhibitors that
target both kinases and microtubules. We further formulate some outstanding questions related to MTA structural biology and present possible routes for
future investigations of this fascinating class of antimitotic agents.

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