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

• Published in: Chembiochem : a European journal of chemical biology Vol. 14; no. 17; pp. 2263 - 2267
• Main Authors: Calvaresi, Emilia C., Granchi, Carlotta, Tuccinardi, Tiziano, Di Bussolo, Valeria, Huigens III, Robert W., Lee, Hyang Yeon, Palchaudhuri, Rahul, Macchia, Marco, Martinelli, Adriano, Minutolo, Filippo, Hergenrother, Paul J.
• Format: Journal Article
• Language: English
• Published: Weinheim WILEY-VCH Verlag 25.11.2013; WILEY‐VCH Verlag; Wiley; Wiley Subscription Services, Inc
• Subjects: Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Biochemistry & Molecular Biology; cancer; Cell Line, Tumor; Cell Proliferation - drug effects; Chemistry, Medicinal; Dose-Response Relationship, Drug; drug design; Drug Screening Assays, Antitumor; Enzyme Inhibitors - chemical synthesis; Enzyme Inhibitors - chemistry; Enzyme Inhibitors - pharmacology; Glucose - chemistry; Glucose - metabolism; glycoconjugation; Glycolysis - drug effects; Humans; L-Lactate Dehydrogenase - antagonists & inhibitors; L-Lactate Dehydrogenase - metabolism; Life Sciences & Biomedicine; Models, Molecular; Molecular Structure; Neoplasms - diagnosis; Neoplasms - drug therapy; Neoplasms - enzymology; Neoplasms - metabolism; Pharmacology & Pharmacy; Science & Technology; Structure-Activity Relationship; targeted anticancer agents; Warburg effect; drug design; glycoconjugation; 1-HOUR INFUSION; LDH-A; GLYCOSYLATION; IDENTIFICATION; HYPOXIA; CELL LUNG-CANCER; PHASE-II TRIAL; AEROBIC GLYCOLYSIS; IN-VIVO; cancer; targeted anticancer agents; EXPRESSION; Warburg effect
• ISSN: 1439-4227; 1439-7633
• DOI: 10.1002/cbic.201300562

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.