Pettersson Ingrid, Ebdrup Søren, Havranek Miroslav, Pihera Pavel, Korínek Marek, Mogensen John P, Jeppesen Claus B, Johansson Eva, Sauerberg Per
Novo Nordisk A/S, Novo Nordisk Park, 2760 Måløv, Denmark.
Bioorg Med Chem Lett. 2007 Aug 15;17(16):4625-9. doi: 10.1016/j.bmcl.2007.05.079. Epub 2007 May 27.
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.
为了设计一种过氧化物酶体增殖物激活受体δ（PPARδ）受体的部分激动剂，采用了基于结构的配体设计方法。在反式激活试验中，最大激活率从87%降至39%。测定了PPARδ受体配体结合域与化合物2复合物的晶体结构，以了解导致最大激活率下降的结构变化。
