Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
6486535 | Biotechnology Advances | 2018 | 36 Pages |
Abstract
Non-steroidal anti-inflammatory drugs (NSAIDs) inhibit prostanoid formation and represent prevalent therapeutics for treatment of inflammatory disorders. However, NSAIDs are afflicted with severe side effects, which might be circumvented by more selective suppression of pro-inflammatory eicosanoid biosynthesis. This concept led to dual inhibitors of microsomal prostaglandin E2 synthase (mPGES)-1 and 5-lipoxygenase that are crucial enzymes in the biosynthesis of pro-inflammatory prostaglandin E2 and leukotrienes. The potential of their dual inhibition in light of superior efficacy and safety is discussed. Focus is placed on natural products, for which direct inhibition of mPGES-1 and leukotriene biosynthesis has been confirmed.
Keywords
Polypharmacologyhydro(pero)xyeicosatetraenoic acidspecialized pro-resolving mediatormPGESMicrosomal prostaglandin E2 synthase-1Microsomal prostaglandin E2 synthaseKBAAKBAEicosanoidCOXSPMABAEpigallocatechin-3-gallateEGCG5-LipoxygenaseH(P)ETEcyclooxygenaseArachidonic acidBoswellic acidPolyunsaturated fatty acidPUFAFlapthromboxanenuclear factorNatural productLeukotrienelipoxygenase5-Lipoxygenase-activating proteinprostaglandin
Related Topics
Physical Sciences and Engineering
Chemical Engineering
Bioengineering
Authors
Andreas Koeberle, Oliver Werz,