Druggable Lipid Signaling Pathways

· Springer Nature
Rafbók
260
Síður
Einkunnir og umsagnir eru ekki staðfestar  Nánar

Um þessa rafbók

Lipids are responsible not just for constituting cellular membrane but also for storing energy, transducing signaling, and modifying proteins. Bioactive lipids, or lipid mediators, transduce signaling as intracellular messenger like phosphoinoitides, and also regulate cell-cell communication through G protein-coupled receptors (GPCRs) that are potentially valuable drug targets in many diseases. Until now, about 40 GPCRs within ~300 rhodopsin-like (class A) GPCRs, are identified as lipid GPCRs. Advances of lipid research have enabled to develop novel small molecules targeting lipid GPCRs for several diseases. Most notably, fingolimod (FTY720), a sphingosine 1-phosphate (S1P) receptor modulator, became the first FDA-approved medicine as an orally bioavailable drug for treating relapsing forms of multiple sclerosis (MS). In addition to fingolimod, other drugs targeting lipid GPCRs had been developed such as latanoprost (prostaglandin F2a analogue, used for ocular hypertension and glaucoma), epoprostenol and treprostinil (prostaglandin I2 analogue, used for pulmonary arterial hypertension), montelukast and pranlukast (cysteinyl leukotriene receptor antagonist, used for asthma and allergies), etc. Novel drugs are also expected like lysophosphatidic acid (LPA) receptor antagonist for treatment of pulmonary fibrosis.

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.

Um höfundinn

Professor Kihara is a Research Assistant Professor at the Sanford Burnham Prebys Medical Discovery Institute in San Diego, California. His translational research is focused on G-protein coupled receptors and their role in disease.

Gefa þessari rafbók einkunn.

Segðu okkur hvað þér finnst.

Upplýsingar um lestur

Snjallsímar og spjaldtölvur
Settu upp forritið Google Play Books fyrir Android og iPad/iPhone. Það samstillist sjálfkrafa við reikninginn þinn og gerir þér kleift að lesa með eða án nettengingar hvar sem þú ert.
Fartölvur og tölvur
Hægt er að hlusta á hljóðbækur sem keyptar eru í Google Play í vafranum í tölvunni.
Lesbretti og önnur tæki
Til að lesa af lesbrettum eins og Kobo-lesbrettum þarftu að hlaða niður skrá og flytja hana yfir í tækið þitt. Fylgdu nákvæmum leiðbeiningum hjálparmiðstöðvar til að flytja skrár yfir í studd lesbretti.