Literature DB >> 26027661

High-throughput screening of antagonists for the orphan G-protein coupled receptor GPR139.

Jia Wang1, Lin-yun Zhu1, Qing Liu1, Morten Hentzer2, Garrick Paul Smith2, Ming-wei Wang1.   

Abstract

AIM: To discover antagonists of the orphan G-protein coupled receptor GPR139 through high-throughput screening of a collection of diverse small molecules.
METHODS: Calcium mobilization assays were used to identify initial hits and for subsequent confirmation studies.
RESULTS: Five small molecule antagonists, representing 4 different scaffolds, were identified following high-throughput screening of 16 000 synthetic compounds.
CONCLUSION: The findings provide important tools for further study of this orphan G-protein coupled receptor.

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Year:  2015        PMID： 26027661      PMCID： PMC4648122          DOI： 10.1038/aps.2015.12

Source DB:  PubMed          Journal:  Acta Pharmacol Sin        ISSN： 1671-4083            Impact factor:   6.150


  10 in total

Review 1.  Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings.

Authors:  C A Lipinski; F Lombardo; B W Dominy; P J Feeney
Journal:  Adv Drug Deliv Rev       Date:  2001-03-01       Impact factor: 15.470

2.  A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays.

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Review 3.  Molecular tinkering of G protein-coupled receptors: an evolutionary success.

Authors:  J Bockaert; J P Pin
Journal:  EMBO J       Date:  1999-04-01       Impact factor: 11.598

4.  Nine new human Rhodopsin family G-protein coupled receptors: identification, sequence characterisation and evolutionary relationship.

Authors:  David E I Gloriam; Helgi B Schiöth; Robert Fredriksson
Journal:  Biochim Biophys Acta       Date:  2005-04-15

5.  Molecular cloning and characterization of a novel Gq-coupled orphan receptor GPRg1 exclusively expressed in the central nervous system.

Authors:  Ayako Matsuo; Shun-ichiro Matsumoto; Mamoru Nagano; Koh-hei Masumoto; Jun Takasaki; Mitsuyuki Matsumoto; Masato Kobori; Masao Katoh; Yasufumi Shigeyoshi
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6.  Characterisation and differential expression of two very closely related G-protein-coupled receptors, GPR139 and GPR142, in mouse tissue and during mouse development.

Authors:  Ute Süsens; Irm Hermans-Borgmeyer; Jens Urny; H Chica Schaller
Journal:  Neuropharmacology       Date:  2005-12-27       Impact factor: 5.250

7.  Identification of surrogate agonists and antagonists for orphan G-protein-coupled receptor GPR139.

Authors:  Liaoyuan A Hu; Pauline M Tang; Nima K Eslahi; Tian Zhou; Joseph Barbosa; Qingyun Liu
Journal:  J Biomol Screen       Date:  2009-06-12

8.  Computer-aided discovery of aromatic l-α-amino acids as agonists of the orphan G protein-coupled receptor GPR139.

Authors:  Vignir Isberg; Kirsten B Andersen; Christoph Bisig; Gunnar P H Dietz; Hans Bräuner-Osborne; David E Gloriam
Journal:  J Chem Inf Model       Date:  2014-05-30       Impact factor: 4.956

9.  Discovery and SAR of a Series of Agonists at Orphan G Protein-Coupled Receptor 139.

Authors:  Feng Shi; Jing Kang Shen; Danqi Chen; Karina Fog; Kenneth Thirstrup; Morten Hentzer; Jens-Jakob Karlsson; Veena Menon; Kenneth A Jones; Kelli E Smith; Garrick Smith
Journal:  ACS Med Chem Lett       Date:  2011-02-28       Impact factor: 4.345

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  10 in total
  9 in total

1.  Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor.

Authors:  Curt A Dvorak; Heather Coate; Diane Nepomuceno; Michelle Wennerholm; Chester Kuei; Brian Lord; David Woody; Pascal Bonaventure; Changlu Liu; Timothy Lovenberg; Nicholas I Carruthers
Journal:  ACS Med Chem Lett       Date:  2015-07-20       Impact factor: 4.345

2.  The orphan receptor GPR139 signals via Gq/11 to oppose opioid effects.

Authors:  Hannah M Stoveken; Stefano Zucca; Ikuo Masuho; Brock Grill; Kirill A Martemyanov
Journal:  J Biol Chem       Date:  2020-06-23       Impact factor: 5.157

3.  Novel Agonist Bioisosteres and Common Structure-Activity Relationships for The Orphan G Protein-Coupled Receptor GPR139.

Authors:  Mohamed A Shehata; Anne C Nøhr; Delphine Lissa; Christoph Bisig; Vignir Isberg; Kirsten B Andersen; Kasper Harpsøe; Fredrik Björkling; Hans Bräuner-Osborne; David E Gloriam
Journal:  Sci Rep       Date:  2016-11-10       Impact factor: 4.379

4.  Re-evaluation of Adrenocorticotropic Hormone and Melanocyte Stimulating Hormone Activation of GPR139 in Vitro.

Authors:  Diane Nepomuceno; Chester Kuei; Curt Dvorak; Timothy Lovenberg; Changlu Liu; Pascal Bonaventure
Journal:  Front Pharmacol       Date:  2018-03-02       Impact factor: 5.810

5.  Systemic and Intra-Habenular Activation of the Orphan G Protein-Coupled Receptor GPR139 Decreases Compulsive-Like Alcohol Drinking and Hyperalgesia in Alcohol-Dependent Rats.

Authors:  Jenni Kononoff; Marsida Kallupi; Adam Kimbrough; Dana Conlisk; Giordano de Guglielmo; Olivier George
Journal:  eNeuro       Date:  2018-07-02

6.  Identification of a novel scaffold for a small molecule GPR139 receptor agonist.

Authors:  Anne Cathrine Nøhr; Mohamed A Shehata; Daniel Palmer; Rina Pokhrel; Maria Vallianou; Simon R Foster; Patrick R Gentry; David E Gloriam; Hans Bräuner-Osborne
Journal:  Sci Rep       Date:  2019-03-07       Impact factor: 4.379

7.  Mutagenesis of GPR139 reveals ways to create gain or loss of function receptors.

Authors:  Lien Wang; Grace Lee; Amy Shih; Chester Kuei; Diane Nepomuceno; Michelle Wennerholm; Frances Fan; Jiejun Wu; Pascal Bonaventure; Timothy W Lovenberg; Changlu Liu
Journal:  Pharmacol Res Perspect       Date:  2019-02-07

8.  The orphan G protein-coupled receptor GPR139 is activated by the peptides: Adrenocorticotropic hormone (ACTH), α-, and β-melanocyte stimulating hormone (α-MSH, and β-MSH), and the conserved core motif HFRW.

Authors:  Anne Cathrine Nøhr; Mohamed A Shehata; Alexander S Hauser; Vignir Isberg; Jacek Mokrosinski; Kirsten B Andersen; I Sadaf Farooqi; Daniel Sejer Pedersen; David E Gloriam; Hans Bräuner-Osborne
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  9 in total

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