Discovery and Optimization of Glucose Uptake Inhibitors

Kevin G. Liu, Ji In Kim, Kellen Olszewski, Anthony M. Barsotti, Koi Morris, Christophe Lamarque, Xuemei Yu, Jack Gaffney, Xiao Jiang Feng, Jeegar P. Patel, Masha V. Poyurovsky

Research output: Contribution to journalArticlepeer-review

18 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)5201-5211
Number of pages11
JournalJournal of Medicinal Chemistry
Volume63
Issue number10
DOIs
StatePublished - May 28 2020
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

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