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 ,
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.
