A Review of Prostanoid Receptors: Expression, Characterization, Regulation, and Mechanism of Action
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REVIEW
A Review of Prostanoid Receptors: Expression, Characterization, Regulation, and Mechanism of Action Roger G. Biringer 1 Received: 25 April 2020 / Accepted: 15 September 2020 # The International CCN Society 2020
Abstract Prostaglandin signaling controls a wide range of biological processes from blood pressure homeostasis to inflammation and resolution thereof to the perception of pain to cell survival. Disruption of normal prostanoid signaling is implicated in numerous disease states. Prostaglandin signaling is facilitated by G-protein-coupled, prostanoid-specific receptors and the array of associated G-proteins. This review focuses on the expression, characterization, regulation, and mechanism of action of prostanoid receptors with particular emphasis on human isoforms. Keywords receptor . prostanoid . eicosanoid . prostaglandin . G-protein . signaling
Introduction Prostaglandins are amphipathic, bioactive signaling molecules derived from the oxidation of arachidonic acid. They are involved in a wide range of roles from homeostasis of blood pressure and blood flow, the initiation and resolution of inflammation, the perception of pain, cell survival, and the progression of numerous disease states. These biomolecules act most often as autocrine or paracrine signaling agents and most have relatively short half-lives. Prostanoid signaling is accomplished through specific G-protein coupled receptors (Figure 1). With the exception of a few isoforms with unknown biological function, all known biologically competent receptors are heptahelical, multi-pass membrane proteins, members of the G-protein coupled receptor 1 family (GPCR) and are among the most abundant membrane proteins (Binda et al. 2004). The diversity of prostanoid action is not only defined by specific receptors and their regulated expression, but also to the diversity of G-proteins that most receptors are able to couple to, leading to actuation of different signaling pathways by the same receptor. Although the actions of these receptors are diverse, many
* Roger G. Biringer [email protected] 1
College of Osteopathic Medicine, Lake Erie College of Osteopathic Medicine, 5000 Lakewood Ranch Blvd, Bradenton, FL 34211, USA
show commonalities in their regulation. Each display agonist-induced desensitization that is usually found to be associated with receptor phosphorylation by various protein kinases. Phosphorylation by G-protein receptor kinases (GRK) can lead to arrestin binding that promotes receptor uptake into clatherin-coated pits leading to sequestration into punctate vesicles. This review focusses primarily on human receptors but discusses receptors from other species when information about the human receptors is lacking.
Prostaglandin D2 Receptors Introduction There are two distinct types of prostaglandin D2 receptors found in humans, the prostanoid DP1 receptor (PGD receptor, PGD2 receptor, Gene: PTGDR) and the DP2 receptor (CRTH2, G-protein coupled receptor 44, CD294, Gene: PTGDR2). Both are coupled to G-proteins and upon binding to PGD2
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