Inducible Prostaglandin E Synthase as a Pharmacological Target for Ischemic Stroke.

ABSTRACT: As the inducible terminal enzyme for prostaglandin E2 (PGE₂) synthesis, microsomal PGE synthase-1 (mPGES-1) contributes to neuroinflammation and secondary brain injury after cerebral ischemia via producing excessive PGE₂. However, a proof of concept that mPGES-1 is a therapeutic target for ischemic stroke has not been established by a pharmacological strategy mainly due to the lack of drug-like mPGES-1 inhibitors that can be used in relevant rodent models. To this end, we recently developed a series of novel small-molecule compounds that can inhibit both human and rodent mPGES-1. In this study, blockade of mPGES-1 by our several novel compounds abolished the lipopolysaccharide (LPS)-induced PGE₂ and pro-inflammatory cytokines interleukin 1β (IL-1β), IL-6, a

SUBMITTER: Li L 

PROVIDER: S-EPMC9130433 | biostudies-literature | 2022 Jan

REPOSITORIES: biostudies-literature