Literature DB >> 17560785

Design of a partial PPARdelta agonist.

Ingrid Pettersson1, Søren Ebdrup, Miroslav Havranek, Pavel Pihera, Marek Korínek, John P Mogensen, Claus B Jeppesen, Eva Johansson, Per Sauerberg.   

Abstract

Structure based ligand design was used in order to design a partial agonist for the PPARdelta receptor. The maximum activation in the transactivation assay was reduced from 87% to 39%. The crystal structure of the ligand binding domain of the PPARdelta receptor in complex with compound 2 was determined in order to understand the structural changes which gave rise to the decrease in maximum activation.

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Year:  2007        PMID: 17560785     DOI: 10.1016/j.bmcl.2007.05.079

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


  2 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.  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

  2 in total

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