Discovery and Optimization of Glucose Uptake Inhibitors
| Autor: | Xuemei Yu, Kellen L. Olszewski, Ji-In Kim, Jack Gaffney, Koi Morris, Christophe Lamarque, Anthony Barsotti, Masha V. Poyurovsky, Jeegar Patel, Kevin Liu, Xiao-Jiang Feng |
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| Rok vydání: | 2020 |
| Předmět: |
Glucose uptake
Glucose Transport Proteins Facilitative Antineoplastic Agents Carbohydrate metabolism 01 natural sciences 03 medical and health sciences Mice Drug Discovery Animals Humans Glycolysis 030304 developmental biology 0303 health sciences biology Dose-Response Relationship Drug Chemistry Glucose transporter 0104 chemical sciences Rats 010404 medicinal & biomolecular chemistry Glucose Biochemistry Caco-2 Anaerobic glycolysis biology.protein Microsomes Liver Molecular Medicine GLUT1 Caco-2 Cells GLUT3 |
| Zdroj: | Journal of medicinal chemistry. 63(10) |
| ISSN: | 1520-4804 |
| Popis: | Aerobic glycolysis, originally identified by Warburg as a hallmark of cancer, has recently been implicated in immune cell activation and growth. Glucose, the starting material for glycolysis, is transported through the cellular membrane by a family of glucose transporters (GLUTs). Therefore, targeting glucose transporters to regulate aerobic glycolysis is an attractive approach to identify potential therapeutic agents for cancers and autoimmune diseases. Herein, we describe the discovery and optimization of a class of potent, orally bioavailable inhibitors of glucose transporters, targeting both GLUT1 and GLUT3. |
| Databáze: | OpenAIRE |
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