First time at Proteopedia? Click on the green links: they change the 3D image. Click and drag the molecules. Proteopedia is a 3D, interactive encyclopedia of proteins, RNA, DNA and other molecules. With a free user account, you can edit pages in Proteopedia. Visit the Main Page to learn more.
|2q5g, resolution 2.70Å ()|
|Gene:||PPARD, NR1C2, PPARB (Homo sapiens)|
Ligand binding domain of PPAR delta receptor in complex with a partial 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 determined in order to understand the structural changes which gave rise to the decrease in maximum activation.
Design of a partial PPARdelta agonist., Pettersson I, Ebdrup S, Havranek M, Pihera P, Korinek M, Mogensen JP, Jeppesen CB, Johansson E, Sauerberg P, Bioorg Med Chem Lett. 2007 Aug 15;17(16):4625-9. Epub 2007 May 27. PMID:17560785
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.