Literature DB >> 21256005

Conformationally constrained farnesoid X receptor (FXR) agonists: heteroaryl replacements of the naphthalene.

Jonathan Y Bass1, Justin A Caravella, Lihong Chen, Katrina L Creech, David N Deaton, Kevin P Madauss, Harry B Marr, Robert B McFadyen, Aaron B Miller, Wendy Y Mills, Frank Navas, Derek J Parks, Terrence L Smalley, Paul K Spearing, Dan Todd, Shawn P Williams, G Bruce Wisely.   

Abstract

To improve on the drug properties of GSK8062 1b, a series of heteroaryl bicyclic naphthalene replacements were prepared. The quinoline 1c was an equipotent FXR agonist with improved drug developability parameters relative to 1b. In addition, analog 1c lowered body weight gain and serum glucose in a DIO mouse model of diabetes.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 21256005     DOI: 10.1016/j.bmcl.2010.12.089

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


  20 in total

1.  Conformational dynamics of human FXR-LBD ligand interactions studied by hydrogen/deuterium exchange mass spectrometry: insights into the antagonism of the hypolipidemic agent Z-guggulsterone.

Authors:  Liping Yang; David Broderick; Yuan Jiang; Victor Hsu; Claudia S Maier
Journal:  Biochim Biophys Acta       Date:  2014-06-18

Review 2.  The significance of the nuclear farnesoid X receptor (FXR) in β cell function.

Authors:  Martina Düfer; Katrin Hörth; Peter Krippeit-Drews; Gisela Drews
Journal:  Islets       Date:  2012-09-01       Impact factor: 2.694

3.  Combining self- and cross-docking as benchmark tools: the performance of DockBench in the D3R Grand Challenge 2.

Authors:  Veronica Salmaso; Mattia Sturlese; Alberto Cuzzolin; Stefano Moro
Journal:  J Comput Aided Mol Des       Date:  2017-08-24       Impact factor: 3.686

Review 4.  FXR signaling in the enterohepatic system.

Authors:  Tsutomu Matsubara; Fei Li; Frank J Gonzalez
Journal:  Mol Cell Endocrinol       Date:  2012-05-17       Impact factor: 4.102

5.  Farnesoid X Receptor Agonist Represses Cytochrome P450 2D6 Expression by Upregulating Small Heterodimer Partner.

Authors:  Xian Pan; Yoon-Kwang Lee; Hyunyoung Jeong
Journal:  Drug Metab Dispos       Date:  2015-04-29       Impact factor: 3.922

Review 6.  Bile acid receptors as targets for the treatment of dyslipidemia and cardiovascular disease.

Authors:  Geoffrey Porez; Janne Prawitt; Barbara Gross; Bart Staels
Journal:  J Lipid Res       Date:  2012-05-01       Impact factor: 5.922

7.  The nuclear receptor FXR uncouples the actions of miR-33 from SREBP-2.

Authors:  Elizabeth J Tarling; Hannah Ahn; Thomas Q de Aguiar Vallim
Journal:  Arterioscler Thromb Vasc Biol       Date:  2015-01-15       Impact factor: 8.311

8.  Bile acid signaling and bariatric surgery.

Authors:  Jingyan Tian; Silvia Huang; Siming Sun; Lili Ding; Eryun Zhang; Wendong Huang
Journal:  Liver Res       Date:  2017-12

9.  Trimethylamine-N-oxide, a metabolite associated with atherosclerosis, exhibits complex genetic and dietary regulation.

Authors:  Brian J Bennett; Thomas Q de Aguiar Vallim; Zeneng Wang; Diana M Shih; Yonghong Meng; Jill Gregory; Hooman Allayee; Richard Lee; Mark Graham; Rosanne Crooke; Peter A Edwards; Stanley L Hazen; Aldons J Lusis
Journal:  Cell Metab       Date:  2013-01-08       Impact factor: 27.287

10.  Ranking docking poses by graph matching of protein-ligand interactions: lessons learned from the D3R Grand Challenge 2.

Authors:  Priscila da Silva Figueiredo Celestino Gomes; Franck Da Silva; Guillaume Bret; Didier Rognan
Journal:  J Comput Aided Mol Des       Date:  2017-08-01       Impact factor: 3.686

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