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Design of a partial PPARdelta agonist

Structure based ligand design was used in order to design a partial agonist for the PPARdelta receptor. The maximum activation in the transactivation assay was reduced from 87% to 39%. The crystal structure of the ligand binding domain of the PPARdelta receptor in complex with compound 2 was determi...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2007-08, Vol.17 (16), p.4625-4629
Main Authors: Pettersson, Ingrid, Ebdrup, Søren, Havranek, Miroslav, Pihera, Pavel, Korínek, Marek, Mogensen, John P, Jeppesen, Claus B, Johansson, Eva, Sauerberg, Per
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Language:English
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Summary:Structure based ligand design was used in order to design a partial agonist for the PPARdelta receptor. The maximum activation in the transactivation assay was reduced from 87% to 39%. The crystal structure of the ligand binding domain of the PPARdelta receptor in complex with compound 2 was determined in order to understand the structural changes which gave rise to the decrease in maximum activation.
ISSN:0960-894X