Targeting microsomal prostaglandin E synthase 1 to develop drugs treating the inflammatory diseases.

Microsomal prostaglandin E synthase 1 (mPGES-1) is the terminal synthase of prostaglandin E2 (PGE2) which plays a crucial role in inflammatory diseases. Thus, mPGES-1 inhibitors are promising agents for their better specificity in blocking the production of PGE2, a potent inflammatory mediator, compared with non-steroidal anti-inflammatory drugs (NSAIDs). Currently, two mPGES-1 inhibitors are undergoing clinical trials and more novel inhibitors are being developed. In this review, we focus on the advances in the development of mPGES-1 inhibitors and the potential of these inhibitors to treat different inflammatory diseases, and discuss the existing challenges. The insights from this review will increase the understanding on the current status of mPGES-1-targeted anti-inflammatory drug development and the potential of these drugs in treating inflammation in diseases.