Literature DB >> 25435151

Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRβ.

Ellen Kick1, Richard Martin2, Yinong Xie2, Brenton Flatt2, Edwin Schweiger2, Tie-Lin Wang2, Brett Busch2, Michael Nyman2, Xiao-Hui Gu2, Grace Yan2, Brandee Wagner2, Max Nanao2, Lam Nguyen2, Thomas Stout2, Artur Plonowski2, Ira Schulman2, Jacek Ostrowski3, Todd Kirchgessner3, Ruth Wexler4, Raju Mohan2.   

Abstract

A series of biaryl pyrazole and imidazole Liver X Receptor (LXR) partial agonists has been synthesized displaying LXRβ selectivity. The LXRβ selective partial agonist 18 was identified with potent induction of ATP binding transporters ABCA1 and ABCG1 in human whole blood (EC50=1.2μM, 55% efficacy). In mice 18 displayed peripheral induction of ABCA1 at 3 and 10mpk doses with no significant elevation of plasma or hepatic triglycerides at these doses, showing an improved profile compared to a full pan-agonist.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  ABCA1; LXR; Liver X Receptor; Nuclear hormone receptor; Partial agonist

Mesh：

Substances：

Year:  2014        PMID： 25435151     DOI： 10.1016/j.bmcl.2014.11.029

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


  9 in total

Review 1.  Liver X receptors link lipid metabolism and inflammation.

Authors:  Ira G Schulman
Journal:  FEBS Lett       Date:  2017-06-13       Impact factor: 4.124

Review 2.  Potential Therapeutic Agents That Target ATP Binding Cassette A1 (ABCA1) Gene Expression.

Authors:  Michael J Haas; Arshag D Mooradian
Journal:  Drugs       Date:  2022-07-21       Impact factor: 11.431

Review 3.  Remembering your A, B, C's: Alzheimer's disease and ABCA1.

Authors:  Cutler T Lewandowski; Megan S Laham; Gregory R J Thatcher
Journal:  Acta Pharm Sin B       Date:  2022-01-24       Impact factor: 14.903

4.  Common and Differential Transcriptional Actions of Nuclear Receptors Liver X Receptors α and β in Macrophages.

Authors:  Ana Ramón-Vázquez; Juan Vladimir de la Rosa; Carlos Tabraue; Felix Lopez; Bonifacio Nicolas Díaz-Chico; Lisardo Bosca; Peter Tontonoz; Susana Alemany; Antonio Castrillo
Journal:  Mol Cell Biol       Date:  2019-02-15       Impact factor: 4.272

5.  Cobalt-Catalyzed Reductive Dimethylcyclopropanation of 1,3-Dienes.

Authors:  Jacob Werth; Christopher Uyeda
Journal:  Angew Chem Int Ed Engl       Date:  2018-09-25       Impact factor: 15.336

Review 6.  Current and future therapies for addressing the effects of inflammation on HDL cholesterol metabolism.

Authors:  Fatima Iqbal; Wendy S Baker; Madiha I Khan; Shwetha Thukuntla; Kevin H McKinney; Nicola Abate; Demidmaa Tuvdendorj
Journal:  Br J Pharmacol       Date:  2017-03-23       Impact factor: 8.739

7.  Discovery of Highly Potent Liver X Receptor β Agonists.

Authors:  Ellen K Kick; Brett B Busch; Richard Martin; William C Stevens; Venkataiah Bollu; Yinong Xie; Brant C Boren; Michael C Nyman; Max H Nanao; Lam Nguyen; Artur Plonowski; Ira G Schulman; Grace Yan; Huiping Zhang; Xiaoping Hou; Meriah N Valente; Rangaraj Narayanan; Kamelia Behnia; A David Rodrigues; Barry Brock; James Smalley; Glenn H Cantor; John Lupisella; Paul Sleph; Denise Grimm; Jacek Ostrowski; Ruth R Wexler; Todd Kirchgessner; Raju Mohan
Journal:  ACS Med Chem Lett       Date:  2016-10-23       Impact factor: 4.345

Review 8.  Ligands of Therapeutic Utility for the Liver X Receptors.

Authors:  Rajesh Komati; Dominick Spadoni; Shilong Zheng; Jayalakshmi Sridhar; Kevin E Riley; Guangdi Wang
Journal:  Molecules       Date:  2017-01-05       Impact factor: 4.411

9.  Structural analysis identifies an escape route from the adverse lipogenic effects of liver X receptor ligands.

Authors:  Anna Y Belorusova; Emma Evertsson; Daniel Hovdal; Jenny Sandmark; Emma Bratt; Ingela Maxvall; Ira G Schulman; Peter Åkerblad; Eva-Lotte Lindstedt
Journal:  Commun Biol       Date:  2019-11-22
  9 in total

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