Literature DB >> 16051104

Nuclear receptor antagonists designed based on the helix-folding inhibition hypothesis.

Yuichi Hashimoto1, Hiroyuki Miyachi.   

Abstract

Here we review our studies on the molecular design of nuclear receptor antagonists, including retinoic acid receptor (RAR) antagonists, retinoid X receptor (RXR) antagonists, androgen receptor (AR) antagonists, and vitamin D receptor (VDR) antagonists, based on inhibition of folding of helix 12, which contains a co-activator binding site. Recent progress in structural development studies of peroxisome proliferator-activated receptor (PPAR) ligands is also reviewed.

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Year:  2005        PMID： 16051104     DOI： 10.1016/j.bmc.2005.03.027

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  11 in total

Review 1.  The retinoid X receptors and their ligands.

Authors:  Marcia I Dawson; Zebin Xia
Journal:  Biochim Biophys Acta       Date:  2011-10-01

Review 2.  Orphan nuclear receptors as targets for drug development.

Authors:  Subhajit Mukherjee; Sridhar Mani
Journal:  Pharm Res       Date:  2010-04-06       Impact factor: 4.200

3.  Circumventing anti-androgen resistance by molecular design.

Authors:  Paula L McGinley; John T Koh
Journal:  J Am Chem Soc       Date:  2007-03-10       Impact factor: 15.419

4.  The unexpected teratogenicity of RXR antagonist UVI3003 via activation of PPARγ in Xenopus tropicalis.

Authors:  Jingmin Zhu; Amanda Janesick; Lijiao Wu; Lingling Hu; Weiyi Tang; Bruce Blumberg; Huahong Shi
Journal:  Toxicol Appl Pharmacol       Date:  2016-11-25       Impact factor: 4.219

5.  From RORγt Agonist to Two Types of RORγt Inverse Agonists.

Authors:  Yonghui Wang; Wei Cai; Ting Tang; Qian Liu; Ting Yang; Liuqing Yang; Yingli Ma; Guifeng Zhang; Yafei Huang; Xiaoxia Song; Lisa A Orband-Miller; Qianqian Wu; Ling Zhou; Zhijun Xiang; Jia-Ning Xiang; Stewart Leung; Liming Shao; Xichen Lin; Mercedes Lobera; Feng Ren
Journal:  ACS Med Chem Lett       Date:  2018-01-22       Impact factor: 4.345

6.  The "Phantom Effect" of the Rexinoid LG100754: structural and functional insights.

Authors:  Yoshiteru Sato; Nick Ramalanjaona; Tiphaine Huet; Noelle Potier; Judit Osz; Pierre Antony; Carole Peluso-Iltis; Pierre Poussin-Courmontagne; Eric Ennifar; Yves Mély; Annick Dejaegere; Dino Moras; Natacha Rochel
Journal:  PLoS One       Date:  2010-11-30       Impact factor: 3.240

7.  Identification of a novel selective PPARγ ligand with a unique binding mode and improved therapeutic profile in vitro.

Authors:  Wei Yi; Jingjing Shi; Guanguan Zhao; X Edward Zhou; Kelly Suino-Powell; Karsten Melcher; H Eric Xu
Journal:  Sci Rep       Date:  2017-01-27       Impact factor: 4.379

8.  Sulfonimide and Amide Derivatives as Novel PPARα Antagonists: Synthesis, Antiproliferative Activity, and Docking Studies.

Authors:  Alessandra Ammazzalorso; Isabella Bruno; Rosalba Florio; Laura De Lellis; Antonio Laghezza; Carmen Cerchia; Barbara De Filippis; Marialuigia Fantacuzzi; Letizia Giampietro; Cristina Maccallini; Paolo Tortorella; Serena Veschi; Fulvio Loiodice; Antonio Lavecchia; Alessandro Cama; Rosa Amoroso
Journal:  ACS Med Chem Lett       Date:  2020-03-03       Impact factor: 4.345

9.  AR mRNA stability is increased with AR-antagonist resistance via 3'UTR variants.

Authors:  D A Dart; K Ashelford; W G Jiang
Journal:  Endocr Connect       Date:  2020-01       Impact factor: 3.335

10.  Structural Development Studies of Subtype-Selective Ligands for Peroxisome Proliferator-Activated Receptors (PPARs) Based on the 3,4-Disubstituted Phenylpropanoic Acid Scaffold as a Versatile Template.

Authors:  Hiroyuki Miyachi; Yuichi Hashimoto
Journal:  PPAR Res       Date:  2008       Impact factor: 4.964
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