MPGES-1 as a target for cancer suppression. A comprehensive invited review "Phospholipase A2 and lipid mediators"

Masako Nakanishi, Vijay Gokhale, Emmanuelle Meuillet, Daniel W. Rosenberg

Research output: Contribution to journalArticle

60 Citations (Scopus)

Abstract

Prostaglandin E2 (PGE2) is a bioactive lipid that can elicit a wide range of biological effects associated with inflammation and cancer. The physiological roles of PGE2 are diverse, mediated in part through activation of key downstream signaling cascades via transmembrane EP receptors located on the cell surface. Elevated levels of COX-2 and concomitant overproduction of PGE2 are often found in human cancers. These observations have led to the use of non-steroidal anti-inflammatory drugs (NSAIDs) as chemopreventive agents, particularly for colorectal cancer (CRC). Their long-term use, however, may be associated with gastrointestinal toxicity and increased risk of adverse cardiovascular events, prompting the development of other enzymatic targets in this pathway. This review will focus on recent efforts to target the terminal synthase, mPGES-1, for cancer chemoprevention. The role of mPGES-1 in the pathogenesis of various cancers is discussed. In addition, an overview of recent efforts to develop small molecule inhibitors that target the protein with high selectivity is also be reviewed.

Original languageEnglish (US)
Pages (from-to)660-664
Number of pages5
JournalBiochimie
Volume92
Issue number6
DOIs
StatePublished - Jun 2010

Fingerprint

Phospholipases A2
Dinoprostone
Lipids
Neoplasms
Toxicity
Chemoprevention
Anti-Inflammatory Agents
Chemical activation
Colorectal Neoplasms
Molecules
Inflammation
Pharmaceutical Preparations
Proteins

Keywords

  • Cancer
  • Inflammation
  • MPGES-1
  • MPGES-1 inhibitor
  • PGE

ASJC Scopus subject areas

  • Biochemistry

Cite this

MPGES-1 as a target for cancer suppression. A comprehensive invited review "Phospholipase A2 and lipid mediators". / Nakanishi, Masako; Gokhale, Vijay; Meuillet, Emmanuelle; Rosenberg, Daniel W.

In: Biochimie, Vol. 92, No. 6, 06.2010, p. 660-664.

Research output: Contribution to journalArticle

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