Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377424 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Ingrid Pettersson, Søren Ebdrup, Miroslav Havranek, Pavel Pihera, Marek Kořínek, John P. Mogensen, Claus B. Jeppesen, Eva Johansson, Per Sauerberg,