دورية أكاديمية

Pregnenolonyl-α-glucoside exhibits marked anti-cancer and CYP17A1 enzymatic inhibitory activities.

التفاصيل البيبلوغرافية
العنوان: Pregnenolonyl-α-glucoside exhibits marked anti-cancer and CYP17A1 enzymatic inhibitory activities.
المؤلفون: Chou, Feng-Pai, Hsu, Wen-Chen, Huang, Sheng-Cih, Chang, Chin-Yuan, Chiou, Ya-Sheng, Tsai, Chia-Tse, Lyu, Jason WenJay, Chen, Wei-Ting, Wu, Tung-Kung
المصدر: Chemical Communications; 2/7/2020, Vol. 56 Issue 11, p1733-1736, 4p
مصطلحات موضوعية: BINDING site assay, GLYCOSIDES, BINDING sites, EXHIBITIONS
مستخلص: We report here that pregnenolonyl-α-glucoside (2), a steryl glycoside synthesized directly from pregnenolone and glucose via a consecutive multienzyme-catalyzed process, exhibits marked dose-dependent cytotoxic activity against HT29, AGS, and ES-2 cells with IC50 values of 23.5 to 50.9 μM. An in vitro CYP17A1 binding pattern assay and protein–ligand docking model support that 2, like abiraterone, binds in the active site heme iron pocket of CYP17A1. [ABSTRACT FROM AUTHOR]
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قاعدة البيانات: Complementary Index
الوصف
تدمد:13597345
DOI:10.1039/c9cc09415f