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The Central Valine Concept Provides an Entry in a New Class of Non Peptide Inhibitors of the P53-MDM2 Interaction

Furet, Pascal and Chene, Patrick and De Pover, Alain and Valat, Therese-Marie and Hergovich Lisztwan, Joanna and Kallen, Joerg and Masuya, Keiichi (2012) The Central Valine Concept Provides an Entry in a New Class of Non Peptide Inhibitors of the P53-MDM2 Interaction. Bioorganic & Medicinal Chemistry Letters.

Abstract

Disrupting the interaction between the p53 tumor suppressor and its regulator MDM2 is a promising therapeutic strategy in anticancer drug research. In our search for non peptide inhibitors of this protein-protein interaction , we have devised a ligand design concept exploiting the central position of Val 93 in the p53 binding pocket of MDM2. The design of molecules based on this concept has allowed us to rapidly identify compounds having a 3-imidazolyl indole core structure as the first representatives of a new class of potent inhibitors of the p53-MDM2 interaction.

Item Type: Article
Additional Information: The material of this paper has already been presented at a conference (CADD Gordon Research Conference 2011, Mount Snow Resort USA-July 2011). Approved OAK ID 5015 project.
Date Deposited: 18 May 2016 23:45
Last Modified: 18 May 2016 23:45
URI: https://oak.novartis.com/id/eprint/6771

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