Discovery and Optimization of Glucose Uptake Inhibitors.
Basic Information
ID: ALA4602704
Journal: J Med Chem
Title: Discovery and Optimization of Glucose Uptake Inhibitors.
Authors: Liu KG, Kim JI, Olszewski K, Barsotti AM, Morris K, Lamarque C, Yu X, Gaffney J, Feng XJ, Patel JP, Poyurovsky MV.
Abstract: 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.
CiteXplore: 32282207
DOI: 10.1021/acs.jmedchem.9b02153
Patent ID: ┄