4LQI

Yeast 20S Proteasome in complex with Vibralactone

4LQI の概要

• エントリーDOI: 10.2210/pdb4lqi/pdb
• 関連するPDBエントリー: 1RYP 2FAK 3E47
• 分子名称: Proteasome subunit alpha type-2, Proteasome subunit beta type-4, Proteasome subunit beta type-5, ... (16 entities in total)
• 機能のキーワード: beta-lactone, inhibitor, natural product, target identification, ntn-protease, cellular protein degradation, hydrolase-hydrolase inhibitor complex, hydrolase/hydrolase inhibitor
• 由来する生物種: Saccharomyces cerevisiae (Baker's yeast); 詳細
• 細胞内の位置: Cytoplasm: P23639 P22141 P30656 P23724 P30657 P38624 P23638 P40303 P32379 P40302 P21242 P21243 P25043 P25451
• タンパク質・核酸の鎖数: 28
• 化学式量合計: 705047.32

構造登録者

List, A.,Zeiler, E.,Gallastegui, N.,Rusch, M.,Hedberg, C.,Sieber, S.A.,Groll, M. (登録日: 2013-07-18, 公開日: 2013-12-25, 最終更新日: 2024-10-30)

主引用文献

List, A.,Zeiler, E.,Gallastegui, N.,Rusch, M.,Hedberg, C.,Sieber, S.A.,Groll, M.
Omuralide and Vibralactone: Differences in the Proteasome-beta-Lactone-gamma-Lactam Binding Scaffold Alter Target Preferences.
Angew.Chem.Int.Ed.Engl., 53:571-574, 2014

PubMed Abstract: Despite their structural similarity, the natural products omuralide and vibralactone have different biological targets. While omuralide blocks the chymotryptic activity of the proteasome with an IC50 value of 47 nM, vibralactone does not have any effect at this protease up to a concentration of 1 mM. Activity-based protein profiling in HeLa cells revealed that the major targets of vibralactone are APT1 and APT2.

PubMed: 24285701
DOI: 10.1002/anie.201308567

実験手法

X-RAY DIFFRACTION (2.7 Å)