Druggable Lipid Signaling Pathways

Drug development targeting lipid signalling pathways are backdated to more than a century, when aspirin was synthesized and selling by Bayer, while the basic mechanism of aspirin's effects (block prostanoid synthesis by inhibiting cyclooxygenases) had not been discovered until 1970s. Nowadays, non-steroidal anti-inflammatory drugs (NSAIDs) like aspirin and ibuprophen are commonly used as antipyretic analgesics and available readily over-the-counter oral drugs. Both upstream and downstream enzymes, such as phospholipase A2s and prostaglandin E synthases, respectively, are also potential therapeutic targets for inflammatory diseases.

Recent studies of lipid metabolism expand the lipid biology field from pro-inflammatory lipid mediators to anti-inflammatory epoxy fatty acids (epoxyeicosatrienoic acids), and also omega-3 fatty acid-derived pro-resolving lipid mediators (lipoxin, resolvin, and neuroprotectin). These bioactive lipids, their metabolic pathways and receptors are of great interest in developing next-generation anti-inflammatory and pro-resolving drugs for a wide variety of diseases including.

This book summarizes not only historical overview of lipid signaling pathways but also provides summary of cutting-edge studies that may provide some hints of novel “druggable” lipid signaling targets.