Literature DB >> 25442311

The identification of GPR3 inverse agonist AF64394; the first small molecule inhibitor of GPR3 receptor function.

Thomas Jensen1, Lisbeth Elster1, Søren Møller Nielsen1, Suresh Babu Poda1, Frosty Loechel1, Christiane Volbracht1, Ib Vestergaard Klewe1, Laurent David1, Stephen P Watson1.   

Abstract

The identification of the novel and selective GPR3 inverse agonist AF64394, the first small molecule inhibitor of GPR3 receptor function, is described. Structure activity relationships and syntheses based around AF64394 are reported.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  AF64394; G protein coupled receptor; GPR12; GPR3; GPR6; Inverse agonist; Orphan receptor

Mesh：

Substances：

Year:  2014        PMID： 25442311     DOI： 10.1016/j.bmcl.2014.09.077

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


  5 in total

1.  Methods for the Development of In Silico GPCR Models.

Authors:  Paula Morales; Dow P Hurst; Patricia H Reggio
Journal:  Methods Enzymol       Date:  2017-07-14       Impact factor: 1.600

2.  Discovery of GSK3β Inhibitors through In Silico Prediction-and-Experiment Cycling Strategy, and Biological Evaluation.

Authors:  Yuno Lee; Sae-Bom Yoon; Hyowon Hong; Hyun Young Kim; Daeyoung Jung; Byoung-San Moon; Woo-Kyu Park; Sunkyung Lee; Hyukjin Kwon; Jihyeong Park; Heeyeong Cho
Journal:  Molecules       Date:  2022-06-14       Impact factor: 4.927

Review 3.  Towards a better understanding of the cannabinoid-related orphan receptors GPR3, GPR6, and GPR12.

Authors:  Paula Morales; Israa Isawi; Patricia H Reggio
Journal:  Drug Metab Rev       Date:  2018-02-01       Impact factor: 4.518

Review 4.  GPR3, GPR6, and GPR12 as novel molecular targets: their biological functions and interaction with cannabidiol.

Authors:  Alyssa S Laun; Sarah H Shrader; Kevin J Brown; Zhao-Hui Song
Journal:  Acta Pharmacol Sin       Date:  2018-06-25       Impact factor: 6.150

5.  Mice lacking GPR3 receptors display late-onset obese phenotype due to impaired thermogenic function in brown adipose tissue.

Authors:  Grzegorz Godlewski; Tony Jourdan; Gergő Szanda; Joseph Tam; Resat Cinar; Judith Harvey-White; Jie Liu; Bani Mukhopadhyay; Pál Pacher; Fong Ming Mo; Douglas Osei-Hyiaman; George Kunos
Journal:  Sci Rep       Date:  2015-10-12       Impact factor: 4.379
  5 in total

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