Design and structure of stapled peptides binding to estrogen receptors

Chris Phillips, Lee R. Roberts, Markus Schade, Richard Bazin, Andrew Bent, Nichola L. Davies, Rob Moore, Andrew D. Pannifer, Andrew R. Pickford, Stephen H. Prior, Christopher M. Read, Andrew Scott, David G. Brown, Bin Xu, Stephen L. Irving

Research output: Contribution to journalArticlepeer-review


Synthetic peptides that specifically bind nuclear hormone receptors offer an alternative approach to small molecules for the modulation of receptor signaling and subsequent gene expression. Here we describe the design of a series of novel stapled peptides that bind the coactivator peptide site of estrogen receptors. Using a number of biophysical techniques, including crystal structure analysis of receptor–stapled peptide complexes, we describe in detail the molecular interactions and demonstrate that all-hydrocarbon staples modulate molecular recognition events. The findings have implications for the design of stapled peptides in general.
Original languageEnglish
Pages (from-to)9696-9699
JournalJournal of the American Chemical Society
Issue number25
Publication statusPublished - 29 Jun 2011


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