Identification and development of mPGES-1 inhibitors: Where we are at?

Hui Hua Chang, Emmanuelle J. Meuillet

Research output: Contribution to journalReview articlepeer-review

81 Scopus citations


Microsomal prostaglandin E synthase-1 (mPGES-1) is the terminal synthase responsible for the synthesis of the pro-tumorigenic prostaglandin E 2 (PGE 2). mPGES-1 is overexpressed in a wide variety of cancers. Since its discovery in 1997 by Bengt Samuelsson and collaborators, the enzyme has been the object of over 200 peer-reviewed articles. Although today mPGES-1 is considered a validated and promising therapeutic target for anticancer drug discovery, challenges in inhibitor design and selectivity are such that up to this date there are only a few published records of small-molecule inhibitors targeting the enzyme and exhibiting some in vivo anticancer activity. This review summarizes the structures, and the in vitro and in vivo activities of these novel mPGES-1 inhibitors. Challenges that have been encountered are also discussed.

Original languageEnglish (US)
Pages (from-to)1909-1934
Number of pages26
JournalFuture Medicinal Chemistry
Issue number15
StatePublished - Nov 2011

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Drug Discovery


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