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Design of a partial PPARdelta agonist |
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| Authors: | Pettersson Ingrid Ebdrup Søren Havranek Miroslav Pihera Pavel Korínek Marek Mogensen John P Jeppesen Claus B Johansson Eva Sauerberg Per |
| Institution: | 1. Novo Nordisk A/S, Novo Nordisk Park, 2760 Måløv, Denmark;2. RE&D VÚFB, s.r.o., Poděbradská 56/186, 180 66 Praha 9, Czech Republic |
| Abstract: | 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. |
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