2YJD

Stapled peptide bound to Estrogen Receptor Beta

2YJD の概要

• エントリーDOI: 10.2210/pdb2yjd/pdb
• 関連するPDBエントリー: 1L2J 1NDE 1QKM 1U3Q 1U3R 1U3S 1U9E 1X76 1X78 1X7B 1X7J 1YY4 1YYE 2FSZ 2JJ3 2LDA 2LDC 2LDD 2YJA 2YLY
• 分子名称: ESTROGEN RECEPTOR BETA, STAPLED PEPTIDE, 4-(2-PROPAN-2-YLOXYBENZIMIDAZOL-1-YL)PHENOL, ... (4 entities in total)
• 機能のキーワード: hormone receptor-peptide complex, hormone receptor/peptide
• 由来する生物種: HOMO SAPIENS (HUMAN); 詳細
• 細胞内の位置: Nucleus : Q92731
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 57466.20

構造登録者

Phillips, C.,Roberts, L.R.,Schade, M.,Bent, A.,Davies, N.L.,Moore, R.,Pannifer, A.D.,Brown, D.G.,Pickford, A.R.,Irving, S.L. (登録日: 2011-05-19, 公開日: 2011-08-03, 最終更新日: 2024-11-20)

主引用文献

Phillips, C.,Roberts, L.R.,Schade, M.,Bazin, R.,Bent, A.,Davies, N.L.,Moore, R.,Pannifer, A.D.,Pickford, A.R.,Prior, S.H.,Read, C.M.,Scott, A.,Brown, D.G.,Xu, B.,Irving, S.L.
Design and Structure of Stapled Peptides Binding to Estrogen Receptors.
J.Am.Chem.Soc., 133:9696-, 2011

PubMed 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.

PubMed: 21612236
DOI: 10.1021/JA202946K

実験手法

X-RAY DIFFRACTION (1.93 Å)