Dual Targeting of the Warburg Effect with a Glucose-Conjugated Lactate Dehydrogenase Inhibitor

被引：49

作者：

Calvaresi, Emilia C. ^{[2
]}

Granchi, Carlotta ^{[3
]}

Tuccinardi, Tiziano ^{[3
]}

Di Bussolo, Valeria ^{[3
]}

Huigens, Robert W., III ^{[1
]}

Lee, Hyang Yeon ^{[1
]}

Palchaudhuri, Rahul ^{[1
]}

Macchia, Marco ^{[3
]}

Martinelli, Adriano ^{[3
]}

Minutolo, Filippo ^{[3
]}

Hergenrother, Paul J. ^{[1
,2
]}

机构：

[1] Univ Illinois, Dept Chem, Urbana, IL 61801 USA

[2] Univ Illinois, Dept Biochem, Urbana, IL 61801 USA

[3] Univ Pisa, Dept Pharm, I-56126 Pisa, Italy

来源：

CHEMBIOCHEM | 2013年 / 14卷 / 17期

基金：

美国国家科学基金会;

关键词：

cancer; drug design; glycoconjugation; targeted anticancer agents; Warburg effect; CELL LUNG-CANCER; PHASE-II TRIAL; LDH-A; AEROBIC GLYCOLYSIS; 1-HOUR INFUSION; IN-VIVO; EXPRESSION; IDENTIFICATION; HYPOXIA; GLYCOSYLATION;

D O I：

10.1002/cbic.201300562

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

070307 [化学生物学]; 071010 [生物化学与分子生物学];

摘要：

Effective glucose diet: We report the development and activity of glucose-conjugated LDH-A inhibitors designed for dual targeting of the Warburg effect (elevated glucose uptake and glycolysis) in cancer cells. Glycoconjugation could be applied to inhibitors of many enzymes involved in glycolysis or tumor metabolism. Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

引用

收藏

页码：2263 / 2267

页数：5

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