β-Peptides with improved affinity for hDM2 and hDMX

…, DS Daniels, DA Guarracino, A Schepartz

Index: Harker, Elizabeth A.; Daniels, Douglas S.; Guarracino, Danielle A.; Schepartz, Alanna Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 5 p. 2038 - 2046

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Citation Number: 50

Abstract

We previously described a series of 314-helical β-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 β- 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 ...