3IUX

Crystal structure of human MDM2 in complex with a potent miniature protein inhibitor (18-residues)

3IUX の概要

• エントリーDOI: 10.2210/pdb3iux/pdb
• 関連するPDBエントリー: 1T4E 1YCR 3EQY 3IVJ
• 分子名称: E3 ubiquitin-protein ligase Mdm2, miniature protein inhibitor, ACETATE ION, ... (5 entities in total)
• 機能のキーワード: mdm2, p53 binding domain, peptide activator of p53, host-virus interaction, ligase, metal-binding, nucleus, phosphoprotein, proto-oncogene, ubl conjugation pathway, zinc-finger
• 細胞内の位置: Nucleus, nucleoplasm: Q00987
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 24806.53

構造登録者

Pazgier, M.,Lu, W. (登録日: 2009-08-31, 公開日: 2009-10-27, 最終更新日: 2023-09-06)

主引用文献

Li, C.,Pazgier, M.,Liu, M.,Lu, W.Y.,Lu, W.
Apamin as a template for structure-based rational design of potent peptide activators of p53.
Angew.Chem.Int.Ed.Engl., 48:8712-8715, 2009

PubMed Abstract: [Image: see text] The oncoproteins MDM2 and MDMX negatively regulate the activity and stability of the tumor suppressor protein p53, and are important molecular targets for anticancer therapy. Grafting four residues critical for MDM2/MDMX binding to the C-terminal α-helix of apamin converts the bee-venom neurotoxin into a novel class of potent p53 activators with potential antitumor activity.

PubMed: 19827079
DOI: 10.1002/anie.200904550

実験手法

X-RAY DIFFRACTION (1.65 Å)