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Eicosanoid receptor information


Most of the eicosanoid receptors are integral membrane protein G protein-coupled receptors (GPCRs) that bind and respond to eicosanoid signaling molecules. Eicosanoids are rapidly metabolized to inactive products and therefore are short-lived. Accordingly, the eicosanoid-receptor interaction is typically limited to a local interaction: cells, upon stimulation, metabolize arachidonic acid to an eicosanoid which then binds cognate receptors on either its parent cell (acting as an autocrine signalling molecule) or on nearby cells (acting as a paracrine signalling molecule) to trigger functional responses within a restricted tissue area, e.g. an inflammatory response to an invading pathogen. In some cases, however, the synthesized eicosanoid travels through the blood (acting as a hormone-like messenger) to trigger systemic or coordinated tissue responses, e.g. prostaglandin (PG) E2 released locally travels to the hypothalamus to trigger a febrile reaction (see Fever § PGE2 release). An example of a non-GPCR receptor that binds many eicosanoids is the PPAR-γ nuclear receptor.[1]

The following is a list of human eicosanoid GPCRs grouped according to the type of eicosanoid ligand that each binds:[2][3]

  1. ^ DuBois RN, Gupta R, Brockman J, Reddy BS, Krakow SL, Lazar MA (1998). "The nuclear eicosanoid receptor, PPAR-γ, is aberrantly expressed in colonic cancers". Carcinogenesis. 19 (1): 49–53. doi:10.1093/carcin/19.1.49. PMID 9472692.
  2. ^ Coleman RA, Smith WL, Narumiya S (1994). "International Union of Pharmacology classification of prostanoid receptors: properties, distribution, and structure of the receptors and their subtypes". Pharmacol. Rev. 46 (2): 205–29. PMID 7938166.
  3. ^ Brink C, Dahlén SE, Drazen J, Evans JF, Hay DW, Nicosia S, Serhan CN, Shimizu T, Yokomizo T (2003). "International Union of Pharmacology XXXVII. Nomenclature for leukotriene and lipoxin receptors". Pharmacol. Rev. 55 (1): 195–227. doi:10.1124/pr.55.1.8. PMID 12615958. S2CID 1584172.

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sequence relationship to the eight other Prostanoid receptors (see Eicosanoid receptor#Prostenoid receptors). DP2 was found to stimulate the directed movement...

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Cysteinyl leukotriene receptor

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represented by GPR99/OXGR1, may constitute a third CysLTR. Leukotriene receptor Eicosanoid receptor Kanaoka Y, Maekawa A, Austen KF (2013). "Identification of GPR99...

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Prostaglandin

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Cannabinoid

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aminoalkylindoles, 1,5-diarylpyrazoles, quinolines, and arylsulfonamides as well as eicosanoids related to endocannabinoids. Medical uses include the treatment of nausea...

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Cysteinyl leukotriene receptor 1

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of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors); whereas GABAB receptors are G protein-coupled...

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Lipid signaling

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coupled receptors (eicosanoid receptors) that largely mediate prostaglandin physiology (although some prostaglandins activate nuclear receptors, see below)...

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Hormone

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different receptors that recognize different hormones and activate the same biochemical pathway. Receptors for most peptide as well as many eicosanoid hormones...

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Muscarinic acetylcholine receptor

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Muscarinic acetylcholine receptors, or mAChRs, are acetylcholine receptors that form G protein-coupled receptor complexes in the cell membranes of certain...

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Prostacyclin

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