947740-21-8Relevant articles and documents
Design of a partial PPARδ agonist
Pettersson, Ingrid,Ebdrup, S?ren,Havranek, Miroslav,Pihera, Pavel,Ko?ínek, Marek,Mogensen, John P.,Jeppesen, Claus B.,Johansson, Eva,Sauerberg, Per
, p. 4625 - 4629 (2007)
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.