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Beta-peptides with improved affinity for hDM2 and hDMX.

Harker, Elizabeth A and Daniels, Douglas and Guarracino, Danielle A and Schepartz, Alanna (2009) Beta-peptides with improved affinity for hDM2 and hDMX. Bioorganic & Medicinal Chemistry, 17 (5). pp. 2038-2046. ISSN 1464-3391

Abstract

We previously described a series of 3(14)-helical beta-peptides that bind the hDM2 protein and inhibit its interaction with a p53-derived peptide in vitro. Here we present a detailed characterization of the interaction of these peptides with hDM2 and report two new beta-peptides in which non-natural side chains have been substituted into the hDM2-recognition epitope. These peptides feature both improved affinity and inhibitory potency in fluorescence polarization and ELISA assays. Additionally, one of the new beta-peptides also binds the hDM2-related protein, hDMX, which has been identified as another key therapeutic target for activation of the p53 pathway in tumors.

Item Type: Article
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Additional Information: Author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: Protein–protein interactions; β-Peptides; Peptidomimetics; Inhibitors; Foldamer; p53; hDM2; Cancer
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Date Deposited: 22 Feb 2010 11:50
Last Modified: 22 Feb 2010 11:50
URI: https://oak.novartis.com/id/eprint/1770

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