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Tebubio's blog - Acting and reacting in life sciences and biotechnologies
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Drug Discovery

Microtubule destabilization by suprafenacine: Template for novel anti-cancer drugs

10/02/2015 by Ali El Baya, PhD No Comments

Recently, B.-H. Choi et al. characterized a novel anti-mitotic molecule termed suprafenacine which destabilizes microtubules, resulting in cell cycle arrest in the G2/M phase and apoptotic cell death.  In silico screening identified several novel anti-cancer molecules based on their ability to inhibit in vitro cell proliferation and tubulin Tubulin cartoonpolymerization.  Structure Activity Relationship studies guided the synthesis of several analogues.  Of these analogues, suprafenacine was the most potent based on its in vitro ability to 1. specifically target cancer cells from multiple tumor types and 2. inhibit tubulin polymerization (IC50 = 0.38 mM). 

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