Prostaglandin-D2 synthase (PGDS) (PGDS)

Prostaglandin-D2 synthase (PGDS) is the primary enzyme responsible for the conversion of prostaglandin H2 (PGH2) into prostaglandin D2 (PGD2), a potent lipid mediator (UniProt: P41222, O60760). There are two distinct isoforms: hematopoietic PGDS (HPGDS), primarily found in mast cells and immune cells, and lipocalin-type PGDS (L-PGDS), found in the central nervous system and cardiovascular system (PubMed: 17503999). PGD2 plays a critical role in the pathogenesis of allergic diseases like asthma and allergic rhinitis by promoting vasodilation, bronchoconstriction, and the recruitment of inflammatory cells (PubMed: 25660364). In the brain, L-PGDS-derived PGD2 is a major endogenous sleep-inducing substance (PubMed: 15155825). Therapeutic strategies targeting PGD2 production focus on inhibiting HPGDS to treat inflammatory and allergic conditions, as well as muscular dystrophy, while avoiding the central effects associated with L-PGDS (PubMed: 28438918). Inhibitors such as TAS-204 and HP-036 are currently being explored for these indications.

Other names

PGD2 synthaseHematopoietic prostaglandin D synthaseLipocalin-type prostaglandin D synthaseHPGDSL-PGDSPTGDSGlutathione-dependent PGD synthaseGlutathione-independent PGD synthase

Inhibition of the enzymatic activity of prostaglandin-D2 synthase, thereby reducing the conversion of prostaglandin H2 to prostaglandin D2.