Design of a partial PPARδ agonist

I Pettersson, S Ebdrup, M Havranek, P Pihera…

文献索引：Pettersson, Ingrid; Ebdrup, Soren; Havranek, Miroslav; Pihera, Pavel; Korinek, Marek; Mogensen, John P.; Jeppesen, Claus B.; Johansson, Eva; Sauerberg, Per Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 16 p. 4625 - 4629

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被引用次数: 15

摘要

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.