Design and Structure of Stapled Peptides Binding to Estrogen Receptors

Phillips, Chris and Roberts, Lee R. and Schade, Markus and Bazin, Richard and Bent, Andrew and Davies, Nichola L. and Moore, Rob and Pannifer, Andrew D. and Pickford, Andrew R. and Prior, Stephen H. and Read, Christopher M. and Scott, Andrew and Brown, David G. and Xu, Bin and Irving, Stephen L. (2011) Design and Structure of Stapled Peptides Binding to Estrogen Receptors. Journal of the American Chemical Society, 133 (25). pp. 9696-9699. ISSN 0002-7863. (The full text of this publication is not available from this repository)

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Official URL
http://dx.doi.org/10.1021/ja202946k

Abstract

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.

Item Type: Article
Subjects: Q Science
Divisions: Faculties > Science Technology and Medical Studies > School of Biosciences
Depositing User: Sue Davies
Date Deposited: 08 Oct 2012 10:58
Last Modified: 30 Jan 2013 09:19
Resource URI: http://kar.kent.ac.uk/id/eprint/31351 (The current URI for this page, for reference purposes)
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