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Issue 4, 2011
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The p53-MDM2/MDMX axis – A chemotype perspective

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Abstract

The protein-protein interaction (PPI) of the tumor suppressor p53 and its negative regulator MDM2 consists of the most intense studied PPI with a group of small molecular weight antagonists described and many more disclosed in patent literature. Due to the Å-level structural insight into p53 interaction with MDM2 there is a reasonable understanding of the requirements of the molecules to bind. In contrast and despite the very close homology and 3-D similarity no potent MDMX antagonist has been disclosed up to date. The current review summarizes the different disclosed chemotypes for MDM2 including a discussion of the cocrystal structures. Structures and approaches to reconstitute functional p53 from mutated p53 are presented. Finally new screening methods and recent biotech deals based on p53 are discussed.

Graphical abstract: The p53-MDM2/MDMX axis – A chemotype perspective

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Publication details

The article was received on 04 Dec 2010, accepted on 13 Jan 2011 and first published on 09 Mar 2011


Article type: Review Article
DOI: 10.1039/C0MD00248H
Citation: Med. Chem. Commun., 2011,2, 246-260
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    The p53-MDM2/MDMX axis – A chemotype perspective

    K. Khoury, G. M. Popowicz, T. A. Holak and A. Dömling, Med. Chem. Commun., 2011, 2, 246
    DOI: 10.1039/C0MD00248H

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