Design of potent PPARalpha agonists.
Article Details
- CitationCopy to clipboard
Sauerberg P, Mogensen JP, Jeppesen L, Bury PS, Fleckner J, Olsen GS, Jeppesen CB, Wulff EM, Pihera P, Havranek M, Polivka Z, Pettersson I
Design of potent PPARalpha agonists.
Bioorg Med Chem Lett. 2007 Jun 1;17(11):3198-202. Epub 2007 Mar 12.
- PubMed ID
- 17379517 [ View in PubMed]
- Abstract
Computational analysis of the ligand binding pocket of the three PPAR receptor subtypes was utilized in the design of potent PPARalpha agonists. Optimum PPARalpha potency and selectivity were obtained with substituents having van der Waals volume around 260. Compound 6 had a PPARalpha potency of 0.002 microM and a selectivity ratio to PPARgamma and PPARdelta of 410 and 2000, respectively.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Rosiglitazone Peroxisome proliferator-activated receptor alpha EC 50 (nM) 4100 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma EC 50 (nM) 200 N/A N/A Details