Scientific background    
     

The NovaSAID drug development programme is based on the 1997 discovery by Per-Johan Jakobsson and Ralf Morgenstern, researchers at the Karolinska Institute, that mPGES-1 is a terminal prostaglandin E synthase.

The enzyme mPGES-1 is essential for the production of Prostaglandin E 2 (PGE2). In inflammation and other related pathological conditions, mPGES-1 catalyses this process leading to increased levels of PGE2. mPGES-1 is the only one of three known PGE synthases that is connected to several pathological conditions such as chronic and acute inflammation, pain, fever, anorexia, atherosclerosis, stroke and cancer.

NSAIDs (such as aspirin, ibuprofen and naproxen) and COX-2 inhibitors (such as Celecoxib), which are presently used to treat inflammation and related pathological conditions, cause gastric ulcerations and cardiovascular side effects. These are believed to be the result of the inhibition of the formation of prostaglandins other than PGE2, the reason being that NSAIDs and Cox-2 inhibitors target a higher level of the arachidonic acid pathway and also depress other prostaglandins, i.e. they are less selective.

 


mPGES-1

 

The inhibition of mPGES-1 is a selective and novel mechanism for the inhibition of the formation of PGE2 and has, therefore, the potential to be of significant value in the treatment of the above mentioned conditions.

   
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