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Since the serendipitous discovery of cisplatin, platinum-based drugs have become well-established antitumor agents, despite the fact that their clinical use is limited by many severe side-effects. In order to both improve the chemotherapeutic index and broaden the therapeutic spectrum of current drugs, our most recent anti-neoplastic agents, Au(III) complexes, were designed as carrier-mediated delivery systems exploiting peptide transporters, which are up-regulated in some cancers. Among all, we focused on two compounds and tested them on human MDA-MB-231 (resistant to cisplatin) breast cancer cell cultures and xenografts, discovering the proteasome as a major target both in vitro and in vivo. 53% inhibition of breast tumor growth in mice was observed after 27 days of treatment at 1.0 mg kgSUP−1 dSUP−1, compared to control. Remarkably, if only the most responsive mice are taken into account, 85% growth inhibition, with some animals showing tumor shrinkage, was observed after 13 days. These results led us to file an international patent, recognizing this class of gold(III) peptidomimetics as suitable candidates for entering phase I clinical trials.


Oncology | Pathology | Pharmacy and Pharmaceutical Sciences


Copyright: © 2014 Nardon et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

supplemental_figures.pdf (43 kB)
List of supplemental figures

Figure_S1.tif (190 kB)
Synthetic scheme (A) for the preparation of dipeptides...

Figure_S2.tif (821 kB)
ROS evaluation

Figure_S3.tif (2538 kB)
Inhibition of proteasome after treatment.

Figure_S4.tif (2862 kB)