Microsomal prostaglandin E synthase-1 (mPGES-1)

Microsomal prostaglandin E synthase‑1 is an inducible membrane-bound enzyme that catalyzes the final step in the formation of prostaglandin E₂ from PGH₂ using glutathione as a cofactor. It is upregulated during inflammation alongside cyclooxygenase‑2 (COX‑2), making it central to pathological increases in PGE₂ associated with pain, fever, arthritis, and certain cancers. Unlike traditional NSAIDs or COXIBs—which block upstream steps affecting multiple eicosanoids—selective inhibition of mPGES–1 offers potential for anti-inflammatory therapy with improved safety due to sparing other physiologically important prostanoids. Its structure reveals unique features within the MAPEG family that support ongoing drug discovery efforts aimed at developing safer anti-inflammatory agents.

Other names

Prostaglandin E synthaseMPGES1PTGES (gene symbol)

Drugs targeting mPGES‑1 act primarily by: - Inhibiting conversion of PGH2 to PGE2, thereby reducing levels of this pro-inflammatory mediator without affecting other prostanoids as broadly as COX inhibitors do. - This selectivity is expected to reduce side effects compared to NSAIDs or COX‑2 inhibitors.