Literature DB >> 21094606

Discovery of isoindoline and tetrahydroisoquinoline derivatives as potent, selective PPARδ agonists.

Christopher A Luckhurst1, Linda A Stein, Mark Furber, Nicola Webb, Marianne J Ratcliffe, Gary Allenby, Sara Botterell, Wendy Tomlinson, Barrie Martin, Andrew Walding.   

Abstract

Small molecule isoindoline and tetrahydroisoquinoline derivatives have been identified as selective agonists of human peroxisome proliferator-activated receptor δ (PPARδ. Compound 18 demonstrated efficacy in a biomarker for increased fatty acid oxidation, with upregulation of pyruvate dehydrogenase kinase, isozyme 4 (PDK4) in human primary myotubes.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 21094606     DOI: 10.1016/j.bmcl.2010.10.117

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


  6 in total

Review 1.  Activation of PPARδ: from computer modelling to biological effects.

Authors:  Shirin Kahremany; Ariela Livne; Arie Gruzman; Hanoch Senderowitz; Shlomo Sasson
Journal:  Br J Pharmacol       Date:  2014-12-15       Impact factor: 8.739

2.  Structural basis for specific ligation of the peroxisome proliferator-activated receptor δ.

Authors:  Chyuan-Chuan Wu; Thomas J Baiga; Michael Downes; James J La Clair; Annette R Atkins; Stephane B Richard; Weiwei Fan; Theresa A Stockley-Noel; Marianne E Bowman; Joseph P Noel; Ronald M Evans
Journal:  Proc Natl Acad Sci U S A       Date:  2017-03-20       Impact factor: 11.205

3.  Left ventricular myocardial contractility is depressed in the borderzone after posterolateral myocardial infarction.

Authors:  Rafael Shimkunas; Zhihong Zhang; Jonathan F Wenk; Mehrdad Soleimani; Michael Khazalpour; Gabriel Acevedo-Bolton; Guanying Wang; David Saloner; Rakesh Mishra; Arthur W Wallace; Liang Ge; Anthony J Baker; Julius M Guccione; Mark B Ratcliffe
Journal:  Ann Thorac Surg       Date:  2013-03-21       Impact factor: 4.330

4.  Rhodium-catalysed tetradehydro-Diels-Alder reactions of enediynes via a rhodium-stabilized cyclic allene.

Authors:  Srinivas Thadkapally; Kaveh Farshadfar; Melanie A Drew; Christopher Richardson; Alireza Ariafard; Stephen G Pyne; Christopher J T Hyland
Journal:  Chem Sci       Date:  2020-09-04       Impact factor: 9.825

5.  Structure-based virtual screening and discovery of New PPARδ/γ dual agonist and PPARδ and γ agonists.

Authors:  Vinicius G Maltarollo; Marie Togashi; Alessandro S Nascimento; Kathia M Honorio
Journal:  PLoS One       Date:  2015-03-13       Impact factor: 3.240

6.  Identification of a Novel PPAR-γ Agonist through a Scaffold Tuning Approach.

Authors:  Hyo Jin Gim; Yong-Sung Choi; Hua Li; Yoon-Jung Kim; Jae-Ha Ryu; Raok Jeon
Journal:  Int J Mol Sci       Date:  2018-10-04       Impact factor: 5.923

  6 in total

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