Literature DB >> 22633688

Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα.

Youseung Shin1, Romain Noel, Subhashis Banerjee, Douglas Kojetin, Xinyi Song, Yuanjun He, Li Lin, Michael D Cameron, Thomas P Burris, Theodore M Kamenecka.   

Abstract

The structure-activity relationship study of a small molecule Rev-erbα agonist is reported. The potency and efficacy of the agonists in a cell-based assay were optimized as compared to the initial lead. Modest mouse pharmacokinetics coupled with an improved in vitro profile make 12e a suitable in vivo probe to interrogate the functions of Rev-erbα in animal models of disease.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID： 22633688      PMCID： PMC3376186          DOI： 10.1016/j.bmcl.2012.04.126

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


  18 in total

1.  Characterization of peripheral circadian clocks in adipose tissues.

Authors:  Sanjin Zvonic; Andrey A Ptitsyn; Steven A Conrad; L Keith Scott; Z Elizabeth Floyd; Gail Kilroy; Xiying Wu; Brian C Goh; Randall L Mynatt; Jeffrey M Gimble
Journal:  Diabetes       Date:  2006-04       Impact factor: 9.461

2.  Rev-erbalpha, a heme sensor that coordinates metabolic and circadian pathways.

Authors:  Lei Yin; Nan Wu; Joshua C Curtin; Mohammed Qatanani; Nava R Szwergold; Robert A Reid; Gregory M Waitt; Derek J Parks; Kenneth H Pearce; G Bruce Wisely; Mitchell A Lazar
Journal:  Science       Date:  2007-11-15       Impact factor: 47.728

3.  Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB.

Authors:  Douglas Kojetin; Yongjun Wang; Theodore M Kamenecka; Thomas P Burris
Journal:  ACS Chem Biol       Date:  2010-11-10       Impact factor: 5.100

4.  Rev-erb beta, a new member of the nuclear receptor superfamily, is expressed in the nervous system during chicken development.

Authors:  E Bonnelye; J M Vanacker; X Desbiens; A Begue; D Stehelin; V Laudet
Journal:  Cell Growth Differ       Date:  1994-12

5.  A serum shock induces circadian gene expression in mammalian tissue culture cells.

Authors:  A Balsalobre; F Damiola; U Schibler
Journal:  Cell       Date:  1998-06-12       Impact factor: 41.582

6.  GSK4112, a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα.

Authors:  Daniel Grant; Lei Yin; Jon L Collins; Derek J Parks; Lisa A Orband-Miller; G Bruce Wisely; Shree Joshi; Mitchell A Lazar; Timothy M Willson; William J Zuercher
Journal:  ACS Chem Biol       Date:  2010-10-15       Impact factor: 5.100

7.  Regulation of adipogenesis by natural and synthetic REV-ERB ligands.

Authors:  Naresh Kumar; Laura A Solt; Yongjun Wang; Pamela M Rogers; Gargi Bhattacharyya; Theodore M Kamenecka; Keith R Stayrook; Christine Crumbley; Z Elizabeth Floyd; Jeffrey M Gimble; Patrick R Griffin; Thomas P Burris
Journal:  Endocrinology       Date:  2010-04-28       Impact factor: 4.736

Review 8.  Nuclear hormone receptors for heme: REV-ERBalpha and REV-ERBbeta are ligand-regulated components of the mammalian clock.

Authors:  Thomas P Burris
Journal:  Mol Endocrinol       Date:  2008-01-24

9.  Identification of heme as the ligand for the orphan nuclear receptors REV-ERBalpha and REV-ERBbeta.

Authors:  Srilatha Raghuram; Keith R Stayrook; Pengxiang Huang; Pamela M Rogers; Amanda K Nosie; Don B McClure; Lorri L Burris; Sepideh Khorasanizadeh; Thomas P Burris; Fraydoon Rastinejad
Journal:  Nat Struct Mol Biol       Date:  2007-11-25       Impact factor: 15.369

10.  Ligand modulation of REV-ERBalpha function resets the peripheral circadian clock in a phasic manner.

Authors:  Qing Jun Meng; Andrew McMaster; Stephen Beesley; Wei Qun Lu; Julie Gibbs; Derek Parks; Jon Collins; Stuart Farrow; Rachelle Donn; David Ray; Andrew Loudon
Journal:  J Cell Sci       Date:  2008-11-01       Impact factor: 5.285
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  8 in total

Review 1.  Nuclear receptor Rev-erbα: up, down, and all around.

Authors:  Logan J Everett; Mitchell A Lazar
Journal:  Trends Endocrinol Metab       Date:  2014-07-22       Impact factor: 12.015

2.  Anti-proliferative actions of a synthetic REV-ERBα/β agonist in breast cancer cells.

Authors:  Yongjun Wang; Douglas Kojetin; Thomas P Burris
Journal:  Biochem Pharmacol       Date:  2015-06-12       Impact factor: 5.858

Review 3.  Recent Progress in the Synthesis of Drugs and Bioactive Molecules Incorporating Nitro(het)arene Core.

Authors:  Maxim Bastrakov; Alexey Starosotnikov
Journal:  Pharmaceuticals (Basel)       Date:  2022-06-03

Review 4.  REV-ERB and ROR nuclear receptors as drug targets.

Authors:  Douglas J Kojetin; Thomas P Burris
Journal:  Nat Rev Drug Discov       Date:  2014-03       Impact factor: 84.694

5.  Pharmacological targeting of the mammalian clock regulates sleep architecture and emotional behaviour.

Authors:  Subhashis Banerjee; Yongjun Wang; Laura A Solt; Kristine Griffett; Melissa Kazantzis; Ariadna Amador; Bahaa M El-Gendy; Salvador Huitron-Resendiz; Amanda J Roberts; Youseung Shin; Theodore M Kamenecka; Thomas P Burris
Journal:  Nat Commun       Date:  2014-12-23       Impact factor: 14.919

6.  In Vitro Metabolic Studies of REV-ERB Agonists SR9009 and SR9011.

Authors:  Lore Geldof; Koen Deventer; Kris Roels; Eva Tudela; Peter Van Eeno
Journal:  Int J Mol Sci       Date:  2016-10-03       Impact factor: 5.923

Review 7.  Recent advances in modulators of circadian rhythms: an update and perspective.

Authors:  Shenzhen Huang; Xinwei Jiao; Dingli Lu; Xiaoting Pei; Di Qi; Zhijie Li
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051

Review 8.  Targeting REV-ERBα for therapeutic purposes: promises and challenges.

Authors:  Shuai Wang; Feng Li; Yanke Lin; Baojian Wu
Journal:  Theranostics       Date:  2020-03-04       Impact factor: 11.556
  8 in total

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