Microsomal prostaglandin E2 synthase-1 inhibitors: a patent review. (2nd September 2017)

• Record Type: Journal Article
• Authors: Psarra, Anastasia; Nikolaou, Aikaterini; Kokotou, Maroula G; Limnios, Dimitris; Kokotos, George
• Is Part Of: Expert opinion on therapeutic patents. Volume 27:Number 9(2017:Sep.)
• Page Start: 1047
• Page End: 1059
• Publication Date: 2017-09-02
• Subjects: Cancer -- inflammation -- inhibitors -- microsomal prostaglandin E2 synthase-1 -- prostaglandin E2; Drugs -- Patents -- Periodicals; 615.10272
• DOI: 10.1080/13543776.2017.1344218
• Languages: English
• ISSNs: 1354-3776

Abstract

ABSTRACT: Introduction : Microsomal prostaglandin E2 synthase-1 (mPGES-1) catalyzes the terminal step of prostaglandin E2 (PGE2 ) generation. It is strongly upregulated in inflamed tissues and overexpressed in tumors and it has been recognized as a key enzyme in inflammatory diseases such as arthritis, atherosclerosis, stroke and cancer. Thus, a great effort has been devoted in developing synthetic mPGES-1 inhibitors as novel anti-inflammatory agents. Areas covered : This review article summarizes the mPGES-1 inhibitors presented in patent literature from 2000 to August 2016 and their biological evaluation, discussing their activities in vitro and in vivo . Expert opinion : The side effects of NSAIDs and COX-2 inhibitors on the gastrointestinal tract and the cardiovascular system showcase the urgent need for the discovery of novel potent and safe anti-inflammatory drugs. mPGES-1 inhibitors may present superior safety in comparison to existing anti-inflammatory drugs. The first synthetic inhibitor of mPGES-1 was reported in 2001 and up to now a variety of structurally different inhibitors has been developed. However, only recently two inhibitors entered clinical trials and none has reached yet the market. More preclinical and clinical studies on mPGES-1 inhibitors are needed to realize if indeed they may become novel agents for the treatment of inflammation and cancer.