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Molecules, Volume 21, Issue 12 (December 2016)
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Cover Story (view full-size image) "Microtubule targeting agents, some of the most effective drugs used in the treatment of cancer, [...] Read more. "Microtubule targeting agents, some of the most effective drugs used in the treatment of cancer, consist of two classes: microtubule stabilizing and destabilizing compounds. We have synthesized and characterized a novel class of compounds that have properties of both microtubule stabilizing and destabilizing drugs. Distinct interactions of these compounds, modeled into the colchicine site on tubulin, suggest novel interactions that may underlie these mixed effects on microtubule structure. The dual effects of these so-called Janus compounds represent a novel phenotype that will provide insights into microtubule dynamics and structure and represent the first class of synthetically tractable small molecules that can elicit microtubule stabilization." View this paper.