title: Design and structure of stapled peptides binding to estrogen receptors.
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.
authors: Department of Chemistry, Pfizer, Sandwich CT13 9NJ, UK. Chris.Phillips@famco.co.uk
authors: Chris
authors: C
authors: Phillips
authors: Lee R
authors: LR
authors: Roberts
authors: Markus
authors: M
authors: Schade
authors: Richard
authors: R
authors: Bazin
authors: Andrew
authors: A
authors: Bent
authors: Nichola L
authors: NL
authors: Davies
authors: Rob
authors: R
authors: Moore
authors: Andrew D
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authors: Pannifer
authors: Andrew R
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authors: Pickford
authors: Stephen H
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authors: Prior
authors: Christopher M
authors: CM
authors: Read
authors: Andrew
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authors: Scott
authors: David G
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authors: Brown
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authors: Xu
authors: Stephen L
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authors: Irving