[Development of anti-inflammatory drugs targeted against prostaglandin-related molecules].
Prostaglandin E2 (PGE2) is a proinflammatory mediator that is synthesized by cyclooxygenases (COX-1 and COX-2) and prostaglandin E synthases (cPGES-1 and mPGES-1); PGE2 exerts its biological effects by binding to specific receptors. Although non-steroidal anti-inflammatory drugs(NSAIDs), which are non-selective COX inhibitors, have been very often used as painkillers, their side effects such as gastrointestinal hemorrhage remain a serious problem. Therefore, the selective COX-2 inhibitors were developed; the use of these inhibitors exerted anti-inflammatory effects without the increased risk of gastrointestinal events. Unfortunately, however, several clinical studies demonstrated that the inhibition of COX-2 was associated with the increased risk of cardiovascular events. Consequently, mPGES-1 and PGE2 receptors are currently expected to be attractive targets for anti-inflammatory drug development in order to reduce the side effects.
Department of Molecular Medical Science, Institute of Medical Science, St. Marianna University School of Medicine.
Tomoo
T
Sato
Toshihiro
T
Nakajima
Yoshihisa
Y
Yamano
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000627:therapeutic use*; D052246:Cyclooxygenase 2 Inhibitors / Q000627:therapeutic use*; D015232:Dinoprostone / Q000096:biosynthesis; D006801:Humans; D019746:Intramolecular Oxidoreductases / Q000037:antagonists & inhibitors*; D058990:Molecular Targeted Therapy; D000071876:Prostaglandin-E Synthases; D018078:Receptors, Prostaglandin E / Q000627:therapeutic use*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D052246:Cyclooxygenase 2 Inhibitors; D018078:Receptors, Prostaglandin E; D019746:Intramolecular Oxidoreductases; C000605862:PTGES protein, human; D000071876:Prostaglandin-E Synthases; D015232:Dinoprostone