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Current Pharmaceutical Design

Editor-in-Chief

ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

Pharmacologic Activation of p53 by Small-Molecule MDM2 Antagonists

Author(s): Hong Shen and Carl G. Maki

Volume 17, Issue 6, 2011

Page: [560 - 568] Pages: 9

DOI: 10.2174/138161211795222603

Price: $65

Abstract

Restoring p53 activity by inhibiting the interaction between p53 and MDM2 represents an attractive approach for cancer therapy. To this end, a number of small-molecule p53-MDM2 binding inhibitors have been developed during the past several years. Nutlin-3 is a potent and selective small-molecule MDM2 antagonist that has shown considerable promise in pre-clinical studies. This review will highlight recent advances in the development of small-molecule MDM2 antagonists as potential cancer therapeutics, with special emphasis on Nutlin-3.

Keywords: Nutlin-3, p53, MDM2, therapy, antagonist, apoptosis, MDMX, p14/ARF, NUTLIN, doxorubicin, therapeutic, choriocarcinoma, Molecular Mechanisms, Antitumor, Perifosine


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