Literature DB >> 17931863

3-Nitro-4-amino benzoic acids and 6-amino nicotinic acids are highly selective agonists of GPR109b.

Philip J Skinner1, Martin C Cherrier, Peter J Webb, Carleton R Sage, Huong T Dang, Cameron C Pride, Ruoping Chen, Susan Y Tamura, Jeremy G Richman, Daniel T Connolly, Graeme Semple.   

Abstract

A series of 3-nitro-4-substituted-aminobenzoic acids were prepared and found to act as potent and highly selective agonists of the orphan human GPCR GPR109b, a low affinity receptor for niacin. No activity was observed at the closely homologous high affinity niacin receptor, GPR109a. A second series, comprising 6-amino-substituted nicotinic acids was, also prepared and several analogues showed comparable activity to the nitroaryl series.

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Year:  2007        PMID: 17931863     DOI: 10.1016/j.bmcl.2007.09.058

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  7 in total

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Authors:  Sarah R Kirk; Adriana L Andrade; Kenneth Melich; Evan P Jackson; Elysia Cuellar; Jeffrey W Karpen
Journal:  Bioorg Med Chem Lett       Date:  2011-08-27       Impact factor: 2.823

2.  Activated human hydroxy-carboxylic acid receptor-3 signals to MAP kinase cascades via the PLC-dependent PKC and MMP-mediated EGFR pathways.

Authors:  Q Zhou; G Li; X Y Deng; X B He; L J Chen; C Wu; Y Shi; K P Wu; L J Mei; J X Lu; N M Zhou
Journal:  Br J Pharmacol       Date:  2012-07       Impact factor: 8.739

3.  Deorphanization of GPR109B as a receptor for the beta-oxidation intermediate 3-OH-octanoic acid and its role in the regulation of lipolysis.

Authors:  Kashan Ahmed; Sorin Tunaru; Claus-Dieter Langhans; Julien Hanson; Christoph W Michalski; Stefan Kölker; Patricia M Jones; Jürgen G Okun; Stefan Offermanns
Journal:  J Biol Chem       Date:  2009-06-26       Impact factor: 5.157

Review 4.  G protein-coupled receptors for energy metabolites as new therapeutic targets.

Authors:  Clara C Blad; Cong Tang; Stefan Offermanns
Journal:  Nat Rev Drug Discov       Date:  2012-07-13       Impact factor: 84.694

5.  Biological roles and therapeutic potential of hydroxy-carboxylic Acid receptors.

Authors:  Kashan Ahmed
Journal:  Front Endocrinol (Lausanne)       Date:  2011-10-25       Impact factor: 5.555

6.  Supplementation of Probiotic Butyricicoccus pullicaecorum Mediates Anticancer Effect on Bladder Urothelial Cells by Regulating Butyrate-Responsive Molecular Signatures.

Authors:  Yen-Chieh Wang; Wei-Chi Ku; Chih-Yi Liu; Yu-Che Cheng; Chih-Cheng Chien; Kang-Wei Chang; Chi-Jung Huang
Journal:  Diagnostics (Basel)       Date:  2021-12-04

Review 7.  Metabolite G-Protein Coupled Receptors in Cardio-Metabolic Diseases.

Authors:  Derek Strassheim; Timothy Sullivan; David C Irwin; Evgenia Gerasimovskaya; Tim Lahm; Dwight J Klemm; Edward C Dempsey; Kurt R Stenmark; Vijaya Karoor
Journal:  Cells       Date:  2021-11-29       Impact factor: 7.666

  7 in total

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