PGE Synthase

PGE synthase inhibitors act on the terminal enzymes that convert prostaglandin H2 into prostaglandin E2. Microsomal prostaglandin E (PGE) synthase-1 (mPGES-1) was described in 1999 as a glutathione-dependent enzyme induced by inflammatory stimuli. Inhibitors of this enzyme reduce prostaglandin E2 formation without blocking the upstream cyclooxygenases. MF63 and mPGES1-IN-3 are mPGES-1 inhibitors for inflammation and pain research. The list also covers the prostaglandin D synthases, which turn the same precursor into prostaglandin D2. Hematopoietic prostaglandin D synthase (H-PGDS) was cloned and its crystal structure solved in 1997. HPGDS inhibitor 1 and hPGDS-IN-1 target H-PGDS, whereas AT 56 inhibits lipocalin-type prostaglandin D synthase (L-PGDS).

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