Glutaminase regulation in cancer cells: a druggable chain of events

Drug Discov Today. 2014 Apr;19(4):450-7. doi: 10.1016/j.drudis.2013.10.008. Epub 2013 Oct 16.

Abstract

Metabolism is the process by which cells convert relatively simple extracellular nutrients into energy and building blocks necessary for their growth and survival. In cancer cells, metabolism is dramatically altered compared with normal cells. These alterations are known as the Warburg effect. One consequence of these changes is cellular addiction to glutamine. Because of this, in recent years the enzyme glutaminase has become a key target for small molecule therapeutic intervention. Like many oncotargets, however, glutaminase has a number of upstream partners that might offer additional druggable targets. This review summarizes the work from the current decade surrounding glutaminase and its regulation, and suggests strategies for therapeutic intervention in relevant cases.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • Glutaminase / antagonists & inhibitors
  • Glutaminase / metabolism*
  • Glutamine / metabolism
  • Humans
  • Neoplasms / drug therapy
  • Neoplasms / metabolism*

Substances

  • Antineoplastic Agents
  • Glutamine
  • Glutaminase