title: Dual targeting of the Warburg effect with a glucose-conjugated lactate dehydrogenase inhibitor.
abstract: 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.
authors.affiliation: Department of Biochemistry, University of Illinois at Urbana-Champaign, 600 S. Mathews Avenue, Urbana, IL 61801 (USA).
authors.forename: Emilia C
authors.initials: EC
authors.lastname: Calvaresi
authors.forename: Carlotta
authors.initials: C
authors.lastname: Granchi
authors.forename: Tiziano
authors.initials: T
authors.lastname: Tuccinardi
authors.forename: Valeria
authors.initials: V
authors.lastname: Di Bussolo
authors.forename: Robert W
authors.initials: RW
authors.lastname: Huigens
authors.forename: Hyang Yeon
authors.initials: HY
authors.lastname: Lee
authors.forename: Rahul
authors.initials: R
authors.lastname: Palchaudhuri
authors.forename: Marco
authors.initials: M
authors.lastname: Macchia
authors.forename: Adriano
authors.initials: A
authors.lastname: Martinelli
authors.forename: Filippo
authors.initials: F
authors.lastname: Minutolo
authors.forename: Paul J
authors.initials: PJ
authors.lastname: Hergenrother
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D005947:Glucose / Q000737:chemistry* / Q000378:metabolism; D006019:Glycolysis / Q000187:drug effects; D006801:Humans; D007770:L-Lactate Dehydrogenase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008958:Models, Molecular; D015394:Molecular Structure; D009369:Neoplasms / Q000175:diagnosis / Q000188:drug therapy* / Q000201:enzymology / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D007770:L-Lactate Dehydrogenase; D005947:Glucose
keywords: Warburg effect; cancer; drug design; glycoconjugation; targeted anticancer agents