Literature DB >> 24900524

Identification of Hydroxybenzoic Acids as Selective Lactate Receptor (GPR81) Agonists with Antilipolytic Effects.

Curt A Dvorak1, Changlu Liu1, Jonathan Shelton1, Chester Kuei1, Steven W Sutton1, Timothy W Lovenberg1, Nicholas I Carruthers1.   

Abstract

Following the characterization of the lactate receptor (GPR81), a focused screening effort afforded 3-hydroxybenzoic acid 1 as a weak agonist of both GPR81 and GPR109a (niacin receptor). An examination of structurally similar arylhydroxy acids led to the identification of 3-chloro-5-hydroxybenzoic acid 2, a selective GPR81 agonist that exhibited favorable in vivo effects on lipolysis in a mouse model of obesity.

Entities:  

Keywords:  FFA; GPR109a; GPR81; HCA1; agonist; flushing; lactate receptor; lipolysis; nicotinic acid receptor

Year:  2012        PMID： 24900524      PMCID： PMC4025785          DOI： 10.1021/ml3000676

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  11 in total

1.  GPR109A (PUMA-G/HM74A) mediates nicotinic acid-induced flushing.

Authors:  Zoltán Benyó; Andreas Gille; Jukka Kero; Marion Csiky; Marie Catherine Suchánková; Rolf M Nüsing; Alexandra Moers; Klaus Pfeffer; Stefan Offermanns
Journal:  J Clin Invest       Date:  2005-12       Impact factor: 14.808

2.  Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).

Authors:  P Douglas Boatman; Thomas O Schrader; Michelle Kasem; Benjamin R Johnson; Philip J Skinner; Jae-Kyu Jung; Jerry Xu; Martin C Cherrier; Peter J Webb; Graeme Semple; Carleton R Sage; Jens Knudsen; Ruoping Chen; Andrew K Taggart; Ester Carballo-Jane; Jeremy G Richman
Journal:  Bioorg Med Chem Lett       Date:  2010-03-20       Impact factor: 2.823

3.  3,5-Dihydroxybenzoic acid, a specific agonist for hydroxycarboxylic acid 1, inhibits lipolysis in adipocytes.

Authors:  Changlu Liu; Chester Kuei; Jessica Zhu; Jingxue Yu; Li Zhang; Amy Shih; Taraneh Mirzadegan; Jonathan Shelton; Steven Sutton; Margery A Connelly; Grace Lee; Nicholas Carruthers; Jiejun Wu; Timothy W Lovenberg
Journal:  J Pharmacol Exp Ther       Date:  2012-03-20       Impact factor: 4.030

4.  Study of GPR81, the lactate receptor, from distant species identifies residues and motifs critical for GPR81 functions.

Authors:  Chester Kuei; Jingxue Yu; Jessica Zhu; Jiejun Wu; Li Zhang; Amy Shih; Taraneh Mirzadegan; Timothy Lovenberg; Changlu Liu
Journal:  Mol Pharmacol       Date:  2011-08-23       Impact factor: 4.436

5.  Nicotinic acid-induced flushing is mediated by activation of epidermal langerhans cells.

Authors:  Zoltán Benyó; Andreas Gille; Clare L Bennett; Björn E Clausen; Stefan Offermanns
Journal:  Mol Pharmacol       Date:  2006-09-28       Impact factor: 4.436

6.  Lactate inhibits lipolysis in fat cells through activation of an orphan G-protein-coupled receptor, GPR81.

Authors:  Changlu Liu; Jiejun Wu; Jessica Zhu; Chester Kuei; Jingxue Yu; Jonathan Shelton; Steven W Sutton; Xiaorong Li; Su Jin Yun; Taraneh Mirzadegan; Curt Mazur; Fredrik Kamme; Timothy W Lovenberg
Journal:  J Biol Chem       Date:  2008-12-01       Impact factor: 5.157

7.  Phenolic acids suppress adipocyte lipolysis via activation of the nicotinic acid receptor GPR109A (HM74a/PUMA-G).

Authors:  Ning Ren; Rebecca Kaplan; Melba Hernandez; Kang Cheng; Lan Jin; Andrew K P Taggart; Amber Y Zhu; Xiaodong Gan; Samuel D Wright; Tian-Quan Cai
Journal:  J Lipid Res       Date:  2009-01-09       Impact factor: 5.922

8.  PUMA-G and HM74 are receptors for nicotinic acid and mediate its anti-lipolytic effect.

Authors:  Sorin Tunaru; Jukka Kero; Annette Schaub; Christian Wufka; Andree Blaukat; Klaus Pfeffer; Stefan Offermanns
Journal:  Nat Med       Date:  2003-02-03       Impact factor: 53.440

9.  Molecular identification of high and low affinity receptors for nicotinic acid.

Authors:  Alan Wise; Steven M Foord; Neil J Fraser; Ashley A Barnes; Nabil Elshourbagy; Michelle Eilert; Diane M Ignar; Paul R Murdock; Klaudia Steplewski; Andrew Green; Andrew J Brown; Simon J Dowell; Philip G Szekeres; David G Hassall; Fiona H Marshall; Shelagh Wilson; Nicholas B Pike
Journal:  J Biol Chem       Date:  2003-01-09       Impact factor: 5.157

10.  Identification of relaxin-3/INSL7 as an endogenous ligand for the orphan G-protein-coupled receptor GPCR135.

Authors:  Changlu Liu; Elo Eriste; Steven Sutton; Jingcai Chen; Barbara Roland; Chester Kuei; Niven Farmer; Hans Jörnvall; Rannar Sillard; Timothy W Lovenberg
Journal:  J Biol Chem       Date:  2003-09-30       Impact factor: 5.157
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  16 in total

1.  Lactate reduces liver and pancreatic injury in Toll-like receptor- and inflammasome-mediated inflammation via GPR81-mediated suppression of innate immunity.

Authors:  Rafaz Hoque; Ahmad Farooq; Ayaz Ghani; Fred Gorelick; Wajahat Zafar Mehal
Journal:  Gastroenterology       Date:  2014-03-20       Impact factor: 22.682

2.  The lactate receptor GPR81 promotes breast cancer growth via a paracrine mechanism involving antigen-presenting cells in the tumor microenvironment.

Authors:  Timothy P Brown; Pushpak Bhattacharjee; Sabarish Ramachandran; Sathish Sivaprakasam; Bojana Ristic; Mohd Omar F Sikder; Vadivel Ganapathy
Journal:  Oncogene       Date:  2020-02-19       Impact factor: 9.867

3.  The Lactate Receptor HCAR1 Modulates Neuronal Network Activity through the Activation of Gα and Gβγ Subunits.

Authors:  Haíssa de Castro Abrantes; Marc Briquet; Céline Schmuziger; Leonardo Restivo; Julien Puyal; Nadia Rosenberg; Anne-Bérengère Rocher; Stefan Offermanns; Jean-Yves Chatton
Journal:  J Neurosci       Date:  2019-03-29       Impact factor: 6.167

Review 4.  Cell-surface G-protein-coupled receptors for tumor-associated metabolites: A direct link to mitochondrial dysfunction in cancer.

Authors:  Bojana Ristic; Yangzom D Bhutia; Vadivel Ganapathy
Journal:  Biochim Biophys Acta Rev Cancer       Date:  2017-05-13       Impact factor: 10.680

5.  Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells.

Authors:  Maja S Engelstoft; Won-Mee Park; Ichiro Sakata; Line V Kristensen; Anna Sofie Husted; Sherri Osborne-Lawrence; Paul K Piper; Angela K Walker; Maria H Pedersen; Mark K Nøhr; Jie Pan; Christopher J Sinz; Paul E Carrington; Taro E Akiyama; Robert M Jones; Cong Tang; Kashan Ahmed; Stefan Offermanns; Kristoffer L Egerod; Jeffrey M Zigman; Thue W Schwartz
Journal:  Mol Metab       Date:  2013-09-04       Impact factor: 7.422

6.  GPR81, a Cell-Surface Receptor for Lactate, Regulates Intestinal Homeostasis and Protects Mice from Experimental Colitis.

Authors:  Punithavathi Ranganathan; Arulkumaran Shanmugam; Daniel Swafford; Amol Suryawanshi; Pushpak Bhattacharjee; Mohamed S Hussein; Pandelakis A Koni; Puttur D Prasad; Zoya B Kurago; Muthusamy Thangaraju; Vadivel Ganapathy; Santhakumar Manicassamy
Journal:  J Immunol       Date:  2018-01-31       Impact factor: 5.422

7.  Involvement of the metabolic sensor GPR81 in cardiovascular control.

Authors:  Kristina Wallenius; Pia Thalén; Jan-Arne Björkman; Petra Johannesson; John Wiseman; Gerhard Böttcher; Ola Fjellström; Nicholas D Oakes
Journal:  JCI Insight       Date:  2017-10-05

8.  Biomimetic Aerobic C-H Olefination of Cyclic Enaminones at Room Temperature: Development toward the Synthesis of 1,3,5-Trisubstituted Benzenes.

Authors:  Yi-Yun Yu; Gunda I Georg
Journal:  Adv Synth Catal       Date:  2014-04-14       Impact factor: 5.837

9.  Hydroxycarboxylic Acid Receptor 1 and Neuroprotection in a Mouse Model of Cerebral Ischemia-Reperfusion.

Authors:  Lara Buscemi; Camille Blochet; Pierre J Magistretti; Lorenz Hirt
Journal:  Front Physiol       Date:  2021-05-21       Impact factor: 4.566

10.  Enhancement of Astroglial Aerobic Glycolysis by Extracellular Lactate-Mediated Increase in cAMP.

Authors:  Nina Vardjan; Helena H Chowdhury; Anemari Horvat; Jelena Velebit; Maja Malnar; Marko Muhič; Marko Kreft; Špela G Krivec; Saša T Bobnar; Katarina Miš; Sergej Pirkmajer; Stefan Offermanns; Gjermund Henriksen; Jon Storm-Mathisen; Linda H Bergersen; Robert Zorec
Journal:  Front Mol Neurosci       Date:  2018-05-08       Impact factor: 5.639
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