GRC
27864 is a potent, selective, orally bioavailable inhibitor of microsomal
prostaglandin E synthase-1 (mPGES-1). Prostaglandins (PGs) are an important
class of lipids related both to physiological and pathological conditions.
Among them, prostaglandin E2 (PGE2) is a key mediator of inflammation, pain and
fever, but it is also important for the protection of the gastrointestinal
mucosa, nutriuresis, blood pressure regulation, and ovulation.
Microsomal
prostaglandin E2 synthase-1 (mPGES-1) catalyzes the terminal step of prostaglandin
E2 (PGE2) generation. mPGES-1 is strongly upregulated in inflamed tissues and
overexpressed in tumors. mPGES-1 inhibitors may be safer anti-inflammatory
agents overcoming the side effects of NSAIDs and COX-2 inhibitors.
GRC
27864 is blessed with single digit nanomolar potency in the recombinant human
mPGES-1 enzyme and in the A549 cellular assays. Moreover, it is shown to be
selective with other prostanoid synthases and was able to effectively regulate
PGE2 biosynthesis in clinically relevant inflammatory settings.
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