Title of article
Design of potent PPARα agonists
Author/Authors
Per Sauerberg، نويسنده , , John P. Mogensen، نويسنده , , Lone Jeppesen، نويسنده , , Paul S. Bury، نويسنده , , Jan Fleckner، نويسنده , , Grith S. Olsen، نويسنده , , Claus B. Jeppesen، نويسنده , , Erik M. Wulff، نويسنده , , Pavel Pihera، نويسنده , , Miroslav Havranek، نويسنده , , Zdenek Polivka، نويسنده , , Ingrid Pettersson ، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
5
From page
3198
To page
3202
Abstract
Computational analysis of the ligand binding pocket of the three PPAR receptor subtypes was utilized in the design of potent PPARα agonists. Optimum PPARα potency and selectivity were obtained with substituents having van der Waals volume around 260. Compound 6 had a PPARα potency of 0.002 μM and a selectivity ratio to PPARγ and PPARδ of 410 and 2000, respectively.
Keywords
PPAR? , agonist , Docking
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798205
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