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Current Cancer Drug Targets


ISSN (Print): 1568-0096
ISSN (Online): 1873-5576

Novel Synthetic Pharmacophores Inducing a Stabilization of Cellular Microtubules

Author(s): Anne Martinez, Emmanuelle Soleilhac, Caroline Barette, Renaud Prudent, Gustavo J. Gozzi, Emilie Vassal-Stermann, Catherine Pillet, Attilio Di Pietro, Marie-Odile Fauvarque and Laurence Lafanechere

Volume 15, Issue 1, 2015

Page: [2 - 13] Pages: 12

DOI: 10.2174/1568009615666141215154149

Price: $65


Microtubule drugs have been widely used in cancer chemotherapies. Although microtubules are subject to regulation by signal transduction mechanisms, their pharmacological modulation has so far relied on compounds that bind to the tubulin subunit. Using a cell-based assay designed to probe the microtubule polymerization status, we identified two pharmacophores, CM09 and CM10, as cell-permeable microtubule stabilizing agents. These synthetic compounds do not affect the assembly state of purified microtubules in vitro but they profoundly suppress microtubule dynamics in vivo. Moreover, they exert cytotoxic effects on several cancer cell lines including multidrug resistant cell lines. Therefore, these classes of compounds represent novel attractive leads for cancer chemotherapy.

Keywords: Chemical biology, high content analysis, microtubule dynamics, microtubule targeting agents, phenotypic screening.

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