Literature DB >> 15857113

Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma.

William J Zuercher1, Stéphanie Gaillard, Lisa A Orband-Miller, Esther Y H Chao, Barry G Shearer, David G Jones, Aaron B Miller, Jon L Collins, Donald P McDonnell, Timothy M Willson.   

Abstract

The first small molecule agonists of the estrogen-related receptors have been identified. GSK4716 (3) and GSK9089 (4) show binding to ERRgamma with remarkable selectivity over the classical estrogen receptors. Notably, in cell-based reporter assays, 3 mimics the protein ligand PGC-1alpha in activation of human ERRbeta and ERRgamma.

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Year:  2005        PMID： 15857113     DOI： 10.1021/jm050161j

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  33 in total

1.  Estrogen-related receptor alpha induces the expression of vascular endothelial growth factor in breast cancer cells.

Authors:  Rebecca A Stein; Stéphanie Gaillard; Donald P McDonnell
Journal:  J Steroid Biochem Mol Biol       Date:  2009-03-03       Impact factor: 4.292

Review 2.  Oestrogen-related receptors in breast cancer: control of cellular metabolism and beyond.

Authors:  Geneviève Deblois; Vincent Giguère
Journal:  Nat Rev Cancer       Date:  2012-11-29       Impact factor: 60.716

Review 3.  The estrogen-related receptors (ERRs): potential targets against bone loss.

Authors:  Ling Zhang; Jiemin Wong; Jean-Marc Vanacker
Journal:  Cell Mol Life Sci       Date:  2016-08-11       Impact factor: 9.261

4.  Regulation of human cytosolic sulfotransferases 1C2 and 1C3 by nuclear signaling pathways in LS180 colorectal adenocarcinoma cells.

Authors:  Elizabeth A Rondini; Hailin Fang; Melissa Runge-Morris; Thomas A Kocarek
Journal:  Drug Metab Dispos       Date:  2013-12-11       Impact factor: 3.922

5.  Neurodevelopmental low-dose bisphenol A exposure leads to early life-stage hyperactivity and learning deficits in adult zebrafish.

Authors:  Katerine S Saili; Margaret M Corvi; Daniel N Weber; Ami U Patel; Siba R Das; Jennifer Przybyla; Kim A Anderson; Robert L Tanguay
Journal:  Toxicology       Date:  2011-11-15       Impact factor: 4.221

6.  Selective identification of hedgehog pathway antagonists by direct analysis of smoothened ciliary translocation.

Authors:  Yu Wang; Anthony C Arvanites; Lance Davidow; Joel Blanchard; Kelvin Lam; Jin Woo Yoo; Shannon Coy; Lee L Rubin; Andrew P McMahon
Journal:  ACS Chem Biol       Date:  2012-05-03       Impact factor: 5.100

7.  Complementary Roles of Estrogen-Related Receptors in Brown Adipocyte Thermogenic Function.

Authors:  Marin L Gantner; Bethany C Hazen; Elodie Eury; Erin L Brown; Anastasia Kralli
Journal:  Endocrinology       Date:  2016-10-20       Impact factor: 4.736

8.  Design, synthesis, and evaluation of simple phenol amides as ERRγ agonists.

Authors:  Hua Lin; Christelle Doebelin; Rémi Patouret; Ruben D Garcia-Ordonez; M R Chang; Venkatasubramanian Dharmarajan; Claudia Ruiz Bayona; Michael D Cameron; Patrick R Griffin; Theodore M Kamenecka
Journal:  Bioorg Med Chem Lett       Date:  2018-03-08       Impact factor: 2.823

9.  Estrogen-related receptor gamma is a key regulator of muscle mitochondrial activity and oxidative capacity.

Authors:  Shamina M Rangwala; Xiaomei Wang; Jennifer A Calvo; Loren Lindsley; Yunyu Zhang; Galina Deyneko; Valerie Beaulieu; Jiaping Gao; Gordon Turner; Judit Markovits
Journal:  J Biol Chem       Date:  2010-04-23       Impact factor: 5.157

10.  Four-dimensional docking: a fast and accurate account of discrete receptor flexibility in ligand docking.

Authors:  Giovanni Bottegoni; Irina Kufareva; Maxim Totrov; Ruben Abagyan
Journal:  J Med Chem       Date:  2009-01-22       Impact factor: 7.446
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