Prostaglandin E1 synthase

Prostaglandin E1 (PGE1) is a bioactive lipid mediator and member of the eicosanoid family synthesized primarily from dihomo-γ-linolenic acid (DGLA) via cyclooxygenase-catalyzed pathways. PGE1 is not synthesized by a unique, specific "PGE1 synthase" enzyme—rather, it is produced through the action of common enzymes of eicosanoid biosynthesis, especially cyclooxygenases, on DGLA (rather than on arachidonic acid, which leads to prostaglandin E2). PGE1 acts locally via G protein-coupled EP receptors (especially EP2 and EP4) and is a potent endogenous vasodilator, inhibitor of platelet aggregation, and has anti-inflammatory, bronchodilatory, and tissue-protective roles. Synthetic PGE1 (alprostadil) and analogues are important therapeutics for conditions such as erectile dysfunction, maintenance of ductus arteriosus patency in neonates, and certain obstetric indications. "Prostaglandin E1 synthesis" is not a conventional, single-molecule drug target but rather describes a biosynthetic pathway involving multiple enzymes. There is no widely recognized enzyme termed "Prostaglandin E1 synthase" as there is for prostaglandin E2 (microsomal prostaglandin E synthase-1); thus, the term is not strictly correct as a canonical drug target.

Other names

Prostaglandin E1 biosynthesisPGE1 synthesisPGE1 production

Activation of G protein-coupled EP receptors (primarily EP2, EP4 subtypes, sometimes EP1/EP3) Increase of intracellular cAMP/cGMP, leading to smooth muscle relaxation and vasodilation Inhibition of platelet aggregation Suppression of inflammatory signaling (inhibition of NF-κB and ROS production)