5WGD

Estrogen Receptor Alpha Ligand Binding Domain in Complex with Estradiol and SRC2-LP1

5WGD の概要

• エントリーDOI: 10.2210/pdb5wgd/pdb
• 分子名称: Estrogen receptor, (ACE)HKILHKLLQDS(NH2), (ACE)AILHKLLQDS(NH2), ... (5 entities in total)
• 機能のキーワード: breast cancer, stapled peptides, synthetic peptides, hormone, transcription
• 由来する生物種: Homo sapiens (Human); 詳細
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 62616.04

構造登録者

Fanning, S.W.,Speltz, T.E.,Mayne, C.G.,Siddiqui, Z.,Greene, G.L.,Tajkhorshid, E.,Moore, T.W. (登録日: 2017-07-14, 公開日: 2018-06-13, 最終更新日: 2024-10-23)

主引用文献

Speltz, T.E.,Mayne, C.G.,Fanning, S.W.,Siddiqui, Z.,Tajkhorshid, E.,Greene, G.L.,Moore, T.W.
A "cross-stitched" peptide with improved helicity and proteolytic stability.
Org. Biomol. Chem., 16:3702-3706, 2018

PubMed Abstract: A new computational approach to obtain quantitative energy profiles for helix folding was used in the design of orthogonal hydrocarbon and lactam bicyclic peptides. The proteolytically stable, "cross-stitched" peptide SRC2-BCP1 shows nanomolar affinity for estrogen receptor α and X-ray crystallography confirms a helical binding pose.

PubMed: 29725689
DOI: 10.1039/c8ob00790j

実験手法

X-RAY DIFFRACTION (1.8 Å)