TITLE

Aspirin metabolites are GPR35 agonists

AUTHOR(S)
Deng, Huayun; Fang, Ye
PUB. DATE
July 2012
SOURCE
Naunyn-Schmiedeberg's Archives of Pharmacology;Jul2012, Vol. 385 Issue 7, p729
SOURCE TYPE
Academic Journal
DOC. TYPE
Article
ABSTRACT
Aspirin is widely used as an anti-inflammatory, anti-platelet, anti-pyretic, and cancer-preventive agent; however, the molecular mode of action is unlikely due entirely to the inhibition of cyclooxygenases. Here, we report the agonist activity of several aspirin metabolites at GPR35, a poorly characterized orphan G protein-coupled receptor. 2,3,5-Trihydroxybenzoic acid, an aspirin catabolite, was found to be the most potent GPR35 agonist among aspirin metabolites. Salicyluric acid, the main metabolite of aspirin, was also active. These results suggest that the GPR35 agonist activity of certain aspirin metabolites may contribute to the clinical features of aspirin.
ACCESSION #
76339074

 

Related Articles

  • Constitutive Activity among Orphan Class-A G Protein Coupled Receptors. Martin, Adam L.; Steurer, Michael A.; Aronstam, Robert S. // PLoS ONE;9/18/2015, Vol. 10 Issue 9, p1 

    The purpose of this study was to evaluate the extent of constitutive activity among orphan class-A G protein coupled receptors within the cAMP signaling pathway. Constitutive signaling was revealed by changes in gene expression under control of the cAMP response element. Gene expression was...

  • Central effects of urotensin-II following ICV administration in rats. Gartlon, Jane; Parker, Frederick; Harrison, David C.; Douglas, Stephen A.; Ashmeade, Tracey E.; Riley, Graham J.; Hughes, Zoe A.; Taylor, Stephen G.; Munton, Richard P.; Hagan, Jim J.; Hunter, Jackie A.; Jones, Declan N.C. // Psychopharmacology;2001, Vol. 155 Issue 4, p426 

    Rationale: Urotensin-II (U-II) has recently been identified as an agonist for the G-protein-coupled receptor, GPR14. Detection of both U-II and GPR14 mRNA in the brain and spinal cord is consistent with a role for U-II in the CNS. However, the effects of central administration of U-II in rodents...

  • Selective Small-Molecule Agonists of G Protein-Coupled Receptor 40 Promote Glucose-Dependent Insulin Secretion and Reduce Blood Glucose in Mice. Tan, Carina P.; Yue Feng; Yun-Ping Zhou; Eiermann, George J.; Petrov, Aleksandr; Zhou, Changyou; Lin, Songnian; Salituro, Gino; Meinke, Peter; Mosley, Ralph; Akiyama, Taro E.; Einstein, Monica; Kumar, Sanjeev; Berger, Joel P.; Mills, Sander G.; Thornberry, Nancy A.; Lihu Yang; Howard, Andrew D. // Diabetes;Aug2008, Vol. 57 Issue 8, p2211 

    OBJECTIVE--Acute activation of G protein-coupled receptor 40 (GPR40) by free fatty acids (FFAs) or synthetic GPR40 agonists enhances insulin secretion. However, it is still a matter of debate whether activation of GPR40 would be beneficial for the treatment of type 2 diabetes, since chronic...

  • N-arachidonoyl glycine, an abundant endogenous lipid, potently drives directed cellular migration through GPR18, the putative abnormal cannabidiol receptor. McHugh, Douglas; Hu, Sherry S. J.; Rimmerman, Neta; Juknat, Ana; Vogel, Zvi; Walker, J. Michael; Bradshaw, Heather B. // BMC Neuroscience;2010, Vol. 11, p44 

    Background: Microglia provide continuous immune surveillance of the CNS and upon activation rapidly change phenotype to express receptors that respond to chemoattractants during CNS damage or infection. These activated microglia undergo directed migration towards affected tissue. Importantly,...

  • GPR40, a free fatty acid receptor, differentially impacts osteoblast behavior depending on differentiation stage and environment. Philippe, Claire; Wauquier, Fabien; Lyan, Bernard; Coxam, Véronique; Wittrant, Yohann // Molecular & Cellular Biochemistry;Jan2016, Vol. 412 Issue 1/2, p197 

    GPR40 is a free fatty acid receptor that has been recently shown to impact bone remodeling. This receptor protects skeleton by inhibiting bone resorbing osteoclast differentiation. Consistent with GPR40 expression on bone forming cells, we assumed that this receptor may also influence osteoblast...

  • The Word 'GPR40 Modulator' May Soon be Entering Our Vocabulary.  // OB/GYN Clinical Alert;Apr2013 Clinical Bries in Primary Care, p2 

    The article discusses a study which reveals the use of G-protein-coupled receptor (GPR40) agonists in lowering glucose levels while maintaining low hypoglycemia risk.

  • The Natural Product Magnolol as a Lead Structure for the Development of Potent Cannabinoid Receptor Agonists. Fuchs, Alexander; Rempel, Viktor; Müller, Christa E. // PLoS ONE;Oct2013, Vol. 8 Issue 10, p1 

    Magnolol (4-allyl-2-(5-allyl-2-hydroxyphenyl)phenol), the main bioactive constituent of the medicinal plant Magnolia officinalis, and its main metabolite tetrahydromagnolol were recently found to activate cannabinoid (CB) receptors. We now investigated the structure-activity relationships of...

  • A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice. Oh, Da Young; Walenta, Evelyn; Akiyama, Taro E; Lagakos, William S; Lackey, Denise; Pessentheiner, Ariane R; Sasik, Roman; Hah, Nasun; Chi, Tyler J; Cox, Jason M; Powels, Mary Ann; Di Salvo, Jerry; Sinz, Christopher; Watkins, Steven M; Armando, Aaron M; Chung, Heekyung; Evans, Ronald M; Quehenberger, Oswald; McNelis, Joanne; Bogner-Strauss, Juliane G // Nature Medicine;Aug2014, Vol. 20 Issue 8, p942 

    It is well known that the ω-3 fatty acids (ω-3-FAs; also known as n-3 fatty acids) can exert potent anti-inflammatory effects. Commonly consumed as fish products, dietary supplements and pharmaceuticals, ω-3-FAs have a number of health benefits ascribed to them, including reduced...

  • Lysophosphatidylinositol Causes Neurite Retraction via GPR55, G13 and RhoA in PC12 Cells. Obara, Yutaro; Ueno, Sanae; Yanagihata, Yoshimi; Nakahata, Norimichi // PLoS ONE;2011, Vol. 6 Issue 8, p1 

    GPR55 was recently identified as a putative receptor for certain cannabinoids, and lysophosphatidylinositol (LPI). Recently, the role of cannabinoids as GPR55 agonists has been disputed by a number of reports, in part, because studies investigating GPR55 often utilized overexpression systems,...

Share

Read the Article

Courtesy of THE LIBRARY OF VIRGINIA

Sorry, but this item is not currently available from your library.

Try another library?
Sign out of this library

Other Topics