2YJA

Stapled Peptides binding to Estrogen Receptor alpha.

2YJA の概要

• エントリーDOI: 10.2210/pdb2yja/pdb
• 関連するPDBエントリー: 1A52 1AKF 1ERE 1ERR 1G50 1GWQ 1GWR 1HCP 1HCQ 1L2I 1PCG 1QKT 1QKU 1R5K 1SJ0 1UOM 1X7E 1X7R 1XP1 1XP6 1XP9 1XPC 1XQC 1YIM 1YIN 1ZKY 2AYR 2B1V 2BJ4 2FAI 2JF9 2JFA 2LDA 2LDC 2LDD 2YAT 2YJD 3ERD 3ERT
• 分子名称: STAPLED PEPTIDE, ESTROGEN RECEPTOR, ESTRADIOL, ... (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: Isoform 1: Nucleus. Isoform 3: Nucleus: P03372
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 30780.33

構造登録者

Phillips, C.,Roberts, L.R.,Schade, M.,Bazin, R.,Bent, A.,Davies, N.L.,Irving, S.L.,Moore, R.,Pannifer, A.D.,Brown, D.G.,Pickford, A.R.,Scott, A.,Xu, B. (登録日: 2011-05-19, 公開日: 2011-08-03, 最終更新日: 2024-11-13)

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 (1.82 Å)