Targeting prostanoid receptors

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An Update on Ligands for Prostanoid Receptors

T he natural prostanoids arise from the activity of intracellular cyclo-oxygenase (COX) on polyunsaturated fatty acids released from membrane phospholipids. In the case of the most important substrate, arachidonic acid (20:4ω6), the first product is prostaglandin G2 (PGG2), which is then reduced to PGH2 by an associated 15-hydroperoxidase [1]. Depending on the tissue, PGH2 may be further metabo...

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Physiology and pathophysiology of prostanoid receptors

Prostanoids, consisting of prostaglandins (PGs) and thromboxanes (TXs), are oxygenated products of C20 unsaturated fatty acids. They include PGD2, PGE2, PGF2 α , PGI2, and TXA2. Given that aspirin-like nonsteroidal anti-inflammatory drugs exert their actions by suppressing prostanoid production, prostanoids have been implicated in processes inhibited by these drugs, including inflammation, feve...

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Prostanoids and prostanoid receptors in signal transduction.

Prostanoids are arachidonic acid metabolites and are generally accepted to play pivotal functions in amongst others inflammation, platelet aggregation, and vasoconstriction/relaxation. Inhibition of their production with, for instance, aspirin has been used for over a century to combat a large variety of pathophysiological processes, with great clinical success. Hence, the cellular changes indu...

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Prostanoid receptors: structures, properties, and functions.

Prostanoids are the cyclooxygenase metabolites of arachidonic acid and include prostaglandin (PG) D(2), PGE(2), PGF(2alpha), PGI(2), and thromboxne A(2). They are synthesized and released upon cell stimulation and act on cells in the vicinity of their synthesis to exert their actions. Receptors mediating the actions of prostanoids were recently identified and cloned. They are G protein-coupled ...

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Characterization of prostanoid receptors in podocytes.

Prostaglandins participate in the regulation of important glomerular functions and are involved in the pathogenesis of glomerular diseases. This study investigates the influence of prostaglandins on membrane voltage, ion conductances, cAMP accumulation, and cytosolic calcium activity ([Ca2+]i) in differentiated podocytes. Prostaglandin E2 (PGE2) caused a concentration-dependent depolarization a...

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ژورنال

عنوان ژورنال: Nature Reviews Drug Discovery

سال: 2009

ISSN: 1474-1776,1474-1784

DOI: 10.1038/nrd2932