3TDD

Crystal structure of yeast CP in complex with Belactosin C

3TDD の概要

• エントリーDOI: 10.2210/pdb3tdd/pdb
• 関連するPDBエントリー: 1RYP 3E47
• 分子名称: Proteasome component Y7, Proteasome component C11, Proteasome component PRE2, ... (16 entities in total)
• 機能のキーワード: ubiquitin, inhibitor, proteasome, drug development, primed substrate binding channel, beta-sandwich flanked by alpha-helices, hydrolase, 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: 705473.70

構造登録者

Korotkov, V.S.,Ludwig, A.,Larionov, O.V.,Lygin, A.V.,Groll, M.,de Meijere, A. (登録日: 2011-08-10, 公開日: 2011-10-12, 最終更新日: 2024-11-20)

主引用文献

Korotkov, V.S.,Ludwig, A.,Larionov, O.V.,Lygin, A.V.,Groll, M.,de Meijere, A.
Synthesis and biological activity of optimized belactosin C congeners.
Org.Biomol.Chem., 9:7791-7798, 2011

PubMed Abstract: Successful biochemical studies of the natural products belactosin A and C as well as their more stable acylated derivatives have proved them to be powerful proteasome inhibitors and thereby potential candidates as pharmacologically relevant active compounds. In order to understand their structure-biological activity relations in detail and to find ways of improving their biological activity, four new modified belactosin congeners have been synthesized and tested. One of them (compound 6) turned out to be a more potent inhibitor against HeLa cells than the known proteasome inhibitor MG132.

PubMed: 21946808
DOI: 10.1039/c1ob05661a

実験手法

X-RAY DIFFRACTION (2.7 Å)