CAY10526 is a selective inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1) expression. CAY10526 potently inhibits PGE2 production in lipopolysaccharide-stimulated RAW 264.7 cells. CAY10526 significantly suppressed tumor growth and increased apoptosis in melanoma xenografts.
selective inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1) expression that potently inhibits PGE2 production
The unique cell biology of Toll-like receptor 4 (TLR4) allows it to initiate two signal-transduction cascades: a signal dependent on the adaptors TIRAP (Mal) and MyD88 that begins at the cell surface and regulates proinflammatory cytokines, and a signal dependent
COX-2 and its product PGE2 enhance carcinogenesis and tumor progression, which has been previously reported in melanoma. As most COX inhibitors cause much toxicity, the downstream microsomal PGE2 synthase-1 (mPGES1) is a consideration for targeting. Human melanoma TMAs were employed
Journal of medicinal chemistry, 50(9), 2176-2184 (2007-04-05)
As a part of our drug discovery effort, recently we clarified the molecular basis of phospholipase A2 (PLA2) inactivation by petrosaspongiolide M (PM), an interesting metabolite belonging to a marine sesterterpene family, containing in its structural architecture a gamma-hydroxybutenolide moiety
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