Author/Authors :
Ingrid Pettersson ، نويسنده , , S?ren Ebdrup، نويسنده , , Miroslav Havranek، نويسنده , , Pavel Pihera، نويسنده , , Marek Ko??nek، نويسنده , , John P. Mogensen، نويسنده , , Claus B. Jeppesen، نويسنده , , Eva Johansson، نويسنده , , Per Sauerberg، نويسنده ,
Abstract :
Structure based ligand design was used in order to design a partial agonist for the PPARδ receptor. The maximum activation in the transactivation assay was reduced from 87% to 39%. The crystal structure of the ligand binding domain of the PPARδ receptor in complex with compound 2 was determined in order to understand the structural changes which gave rise to the decrease in maximum activation.
Keywords :
PPARd , Partial , Docking , design , agonist
