Literature DB >> 26396690

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

Curt A Dvorak1, Heather Coate1, Diane Nepomuceno1, Michelle Wennerholm1, Chester Kuei1, Brian Lord1, David Woody1, Pascal Bonaventure1, Changlu Liu1, Timothy Lovenberg1, Nicholas I Carruthers1.   

Abstract

A focused high throughput screening for GPR139 was completed for a select 100K compounds, and new agonist leads were identified. Subsequent analysis and structure-activity relationship studies identified (S)-3-chloro-N-(2-oxo-2-((1-phenylethyl)amino)ethyl)benzamide 7c as a potent and selective agonist of hGPR139 with an EC50 = 16 nM. The compound was found to cross the blood-brain barrier and have good drug-like properties amenable for oral dosing in rat.

Entities:  

Keywords:  GPR139; Orphan receptors; agonists; glycine amides

Year:  2015        PMID： 26396690      PMCID： PMC4569879          DOI： 10.1021/acsmedchemlett.5b00247

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


  10 in total

1.  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

2.  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
Journal:  Biochem Biophys Res Commun       Date:  2005-05-27       Impact factor: 3.575

3.  Reductive Amination of Aldehydes and Ketones with Sodium Triacetoxyborohydride. Studies on Direct and Indirect Reductive Amination Procedures(1).

Authors:  Ahmed F. Abdel-Magid; Kenneth G. Carson; Bruce D. Harris; Cynthia A. Maryanoff; Rekha D. Shah
Journal:  J Org Chem       Date:  1996-05-31       Impact factor: 4.354

4.  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

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

Authors:  Jia Wang; Lin-yun Zhu; Qing Liu; Morten Hentzer; Garrick Paul Smith; Ming-wei Wang
Journal:  Acta Pharmacol Sin       Date:  2015-06-01       Impact factor: 6.150

6.  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

7.  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

8.  Aminopyrazole-Phenylalanine Based GPR142 Agonists: Discovery of Tool Compound and in Vivo Efficacy Studies.

Authors:  Ming Yu; Mike Lizarzaburu; Alykhan Motani; Zice Fu; Xiaohui Du; Jiwen Jim Liu; Xianyun Jiao; SuJen Lai; Peter Fan; Angela Fu; Qingxiang Liu; Michiko Murakoshi; Futoshi Nara; Kozo Oda; Ryo Okuyama; Jeff D Reagan; Nobuaki Watanabe; Mami Yamazaki; Yumei Xiong; Ying Zhang; Run Zhuang; Daniel C-H Lin; Jonathan B Houze; Julio C Medina; Leping Li
Journal:  ACS Med Chem Lett       Date:  2013-05-01       Impact factor: 4.345

9.  Novel human G-protein-coupled receptors.

Authors:  William B Vanti; Tuan Nguyen; Regina Cheng; Kevin R Lynch; Susan R George; Brian F O'Dowd
Journal:  Biochem Biophys Res Commun       Date:  2003-05-23       Impact factor: 3.575

10.  Stereodivergent synthesis of chiral fullerenes by [3 + 2] cycloadditions to C₆₀.

Authors:  Enrique E Maroto; Salvatore Filippone; Margarita Suárez; Roberto Martínez-Álvarez; Abel de Cózar; Fernando P Cossío; Nazario Martín
Journal:  J Am Chem Soc       Date:  2014-01-03       Impact factor: 15.419
  10 in total
  12 in total

1.  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

2.  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

3.  The GPR139 reference agonists 1a and 7c, and tryptophan and phenylalanine share a common binding site.

Authors:  Anne Cathrine Nøhr; Willem Jespers; Mohamed A Shehata; Leonard Floryan; Vignir Isberg; Kirsten Bayer Andersen; Johan Åqvist; Hugo Gutiérrez-de-Terán; Hans Bräuner-Osborne; David E Gloriam
Journal:  Sci Rep       Date:  2017-04-25       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 role of orphan receptor GPR139 in neuropsychiatric behavior.

Authors:  Maria Dao; Hannah M Stoveken; Yan Cao; Kirill A Martemyanov
Journal:  Neuropsychopharmacology       Date:  2021-01-21       Impact factor: 8.294

9.  Protection of Primary Dopaminergic Midbrain Neurons by GPR139 Agonists Supports Different Mechanisms of MPP(+) and Rotenone Toxicity.

Authors:  Kirsten Bayer Andersen; Jens Leander Johansen; Morten Hentzer; Garrick Paul Smith; Gunnar P H Dietz
Journal:  Front Cell Neurosci       Date:  2016-06-28       Impact factor: 5.505

10.  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
Journal:  Neurochem Int       Date:  2016-12-01       Impact factor: 3.921
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