Design of a partial PPARdelta agonist.
Article Details
- CitationCopy to clipboard
Pettersson I, Ebdrup S, Havranek M, Pihera P, Korinek M, Mogensen JP, Jeppesen CB, Johansson E, Sauerberg P
Design of a partial PPARdelta agonist.
Bioorg Med Chem Lett. 2007 Aug 15;17(16):4625-9. Epub 2007 May 27.
- PubMed ID
- 17560785 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Polypeptides
Name UniProt ID Peroxisome proliferator-activated receptor delta Q03181 Details - Binding Properties
Drug Target Property Measurement pH Temperature (°C) Cardarine Peroxisome proliferator-activated receptor alpha EC 50 (nM) 3900 N/A N/A Details Cardarine Peroxisome proliferator-activated receptor delta EC 50 (nM) 8 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor alpha EC 50 (nM) >10000 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma EC 50 (nM) 300 N/A N/A Details