Literature DB >> 27326330

Design and Synthesis of 2-Alkylpyrimidine-4,6-diol and 6-Alkylpyridine-2,4-diol as Potent GPR84 Agonists.

Yang Liu1, Qing Zhang2, Lin-Hai Chen3, Hui Yang4, Wei Lu1, Xin Xie5, Fa-Jun Nan3.   

Abstract

A series of alkylpyrimidine-4,6-diol derivatives were designed and synthesized as novel GRP84 agonists based on a high-throughput screening (HTS) hit 1. 6-Nonylpyridine-2,4-diol was identified as the most potent agonist of GPR84 reported so far, with an EC50 of 0.189 nM. These novel GPR84 agonists will provide valuable tools for the study of the physiological functions of GPR84.

Entities:  

Keywords:  2-alkylpyrimidine-4,6-diol; 6-alkylpyridine-2,4-diol; GPR84; agonists; structural modification

Year:  2016        PMID： 27326330      PMCID： PMC4904254          DOI： 10.1021/acsmedchemlett.6b00025

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


  18 in total

1.  Medium-chain fatty acids as ligands for orphan G protein-coupled receptor GPR84.

Authors:  Jinghong Wang; Xiaosu Wu; Nicole Simonavicius; Hui Tian; Lei Ling
Journal:  J Biol Chem       Date:  2006-09-11       Impact factor: 5.157

2.  The role of G-protein receptor 84 in experimental neuropathic pain.

Authors:  Louise S C Nicol; John M Dawes; Federica La Russa; Athanasios Didangelos; Anna K Clark; Clive Gentry; John Grist; John B Davies; Marzia Malcangio; Stephen B McMahon
Journal:  J Neurosci       Date:  2015-06-10       Impact factor: 6.167

3.  GPR84 deficiency reduces microgliosis, but accelerates dendritic degeneration and cognitive decline in a mouse model of Alzheimer's disease.

Authors:  Julie Audoy-Rémus; Lusine Bozoyan; Aline Dumas; Mohammed Filali; Cynthia Lecours; Steve Lacroix; Serge Rivest; Marie-Eve Tremblay; Luc Vallières
Journal:  Brain Behav Immun       Date:  2015-01-28       Impact factor: 7.217

4.  GPR84 sustains aberrant β-catenin signaling in leukemic stem cells for maintenance of MLL leukemogenesis.

Authors:  Philipp A Dietrich; Chen Yang; Halina H L Leung; Jennifer R Lynch; Estrella Gonzales; Bing Liu; Michelle Haber; Murray D Norris; Jianlong Wang; Jenny Yingzi Wang
Journal:  Blood       Date:  2014-10-07       Impact factor: 22.113

5.  GPR84 and TREM-1 Signaling Contribute to the Pathogenesis of Reflux Esophagitis.

Authors:  Heba Abdel-Aziz; Mathias Schneider; Winfried Neuhuber; Abdel Meguid Kassem; Saleem Khailah; Jürgen Müller; Hadeel Gamal Eldeen; Ahmed Khairy; Mohamed T Khayyal; Anastasiia Shcherbakova; Thomas Efferth; Gudrun Ulrich-Merzenich
Journal:  Mol Med       Date:  2016-05-09       Impact factor: 6.354

6.  Medium-chain fatty acid-sensing receptor, GPR84, is a proinflammatory receptor.

Authors:  Masakatsu Suzuki; Sachiko Takaishi; Miyuki Nagasaki; Yoshiko Onozawa; Ikue Iino; Hiroaki Maeda; Tomoaki Komai; Tomiichiro Oda
Journal:  J Biol Chem       Date:  2013-02-28       Impact factor: 5.157

Review 7.  Free fatty acids-sensing G protein-coupled receptors in drug targeting and therapeutics.

Authors:  Tomo Yonezawa; Riho Kurata; Kaori Yoshida; Masanori A Murayama; Xiaofeng Cui; Akihiko Hasegawa
Journal:  Curr Med Chem       Date:  2013       Impact factor: 4.530

8.  G protein-coupled receptor 84, a microglia-associated protein expressed in neuroinflammatory conditions.

Authors:  Caroline Bouchard; Julie Pagé; Andréanne Bédard; Pierrot Tremblay; Luc Vallières
Journal:  Glia       Date:  2007-06       Impact factor: 7.452

9.  A medium-chain fatty acid receptor Gpr84 in zebrafish: expression pattern and roles in immune regulation.

Authors:  Qiaoyan Huang; Dong Feng; Kai Liu; Peng Wang; Hongyan Xiao; Ying Wang; Shicui Zhang; Zhenhui Liu
Journal:  Dev Comp Immunol       Date:  2014-04-01       Impact factor: 3.636

10.  Expression analysis of G Protein-Coupled Receptors in mouse macrophages.

Authors:  Jane E Lattin; Kate Schroder; Andrew I Su; John R Walker; Jie Zhang; Tim Wiltshire; Kaoru Saijo; Christopher K Glass; David A Hume; Stuart Kellie; Matthew J Sweet
Journal:  Immunome Res       Date:  2008-04-29
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  12 in total

Review 1.  Neuro-psychopharmacological perspective of Orphan receptors of Rhodopsin (class A) family of G protein-coupled receptors.

Authors:  Muhammad Zahid Khan; Ling He
Journal:  Psychopharmacology (Berl)       Date:  2017-03-13       Impact factor: 4.530

2.  The Two Formyl Peptide Receptors Differently Regulate GPR84-Mediated Neutrophil NADPH Oxidase Activity.

Authors:  Jonas Mårtensson; Martina Sundqvist; Asmita Manandhar; Loukas Ieremias; Linjie Zhang; Trond Ulven; Xin Xie; Lena Björkman; Huamei Forsman
Journal:  J Innate Immun       Date:  2021-03-31       Impact factor: 7.349

3.  Regulation of mitochondrial metabolism in murine skeletal muscle by the medium-chain fatty acid receptor Gpr84.

Authors:  Magdalene K Montgomery; Brenna Osborne; Amanda E Brandon; Liam O'Reilly; Corrine E Fiveash; Simon H J Brown; Brendan P Wilkins; Azrah Samsudeen; Josephine Yu; Beena Devanapalli; Ashley Hertzog; Adviye A Tolun; Tomas Kavanagh; Antony A Cooper; Todd W Mitchell; Trevor J Biden; Nicola J Smith; Gregory J Cooney; Nigel Turner
Journal:  FASEB J       Date:  2019-08-15       Impact factor: 5.834

4.  Three classes of ligands each bind to distinct sites on the orphan G protein-coupled receptor GPR84.

Authors:  Zobaer Al Mahmud; Laura Jenkins; Trond Ulven; Frédéric Labéguère; Romain Gosmini; Steve De Vos; Brian D Hudson; Irina G Tikhonova; Graeme Milligan
Journal:  Sci Rep       Date:  2017-12-20       Impact factor: 4.379

5.  Activation of the Immune-Metabolic Receptor GPR84 Enhances Inflammation and Phagocytosis in Macrophages.

Authors:  Carlota Recio; Daniel Lucy; Gareth S D Purvis; Poppy Iveson; Lynda Zeboudj; Asif J Iqbal; Daniel Lin; Chris O'Callaghan; Lucy Davison; Esther Griesbach; Angela J Russell; Graham M Wynne; Lea Dib; Claudia Monaco; David R Greaves
Journal:  Front Immunol       Date:  2018-06-20       Impact factor: 7.561

6.  6-(Ar)Alkylamino-Substituted Uracil Derivatives: Lipid Mimetics with Potent Activity at the Orphan G Protein-Coupled Receptor 84 (GPR84).

Authors:  Thanigaimalai Pillaiyar; Meryem Köse; Vigneshwaran Namasivayam; Katharina Sylvester; Gleice Borges; Dominik Thimm; Ivar von Kügelgen; Christa E Müller
Journal:  ACS Omega       Date:  2018-03-20

7.  On-target and off-target effects of novel orthosteric and allosteric activators of GPR84.

Authors:  Sarah J Mancini; Zobaer Al Mahmud; Laura Jenkins; Daniele Bolognini; Robert Newman; Matt Barnes; Michelle E Edye; Stephen B McMahon; Andrew B Tobin; Graeme Milligan
Journal:  Sci Rep       Date:  2019-02-12       Impact factor: 4.379

Review 8.  A Recent Achievement In the Discovery and Development of Novel Targets for the Treatment of Type-2 Diabetes Mellitus.

Authors:  Tafere Mulaw Belete
Journal:  J Exp Pharmacol       Date:  2020-01-10

Review 9.  Therapeutic validation of an orphan G protein-coupled receptor: The case of GPR84.

Authors:  Sara Marsango; Natasja Barki; Laura Jenkins; Andrew B Tobin; Graeme Milligan
Journal:  Br J Pharmacol       Date:  2020-09-17       Impact factor: 9.473

10.  Synthesis and Pharmacological Evaluation of Triazolopyrimidinone Derivatives as Noncompetitive, Intracellular Antagonists for CC Chemokine Receptors 2 and 5.

Authors:  Natalia V Ortiz Zacarías; Jacobus P D van Veldhoven; Lisa S den Hollander; Burak Dogan; Joseph Openy; Ya-Yun Hsiao; Eelke B Lenselink; Laura H Heitman; Adriaan P IJzerman
Journal:  J Med Chem       Date:  2019-12-13       Impact factor: 7.446
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