Structure-activity relationships of dimeric PPAR agonists.
Article Details
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Sauerberg P, Mogensen JP, Jeppesen L, Svensson LA, Fleckner J, Nehlin J, Wulff EM, Pettersson I
Structure-activity relationships of dimeric PPAR agonists.
Bioorg Med Chem Lett. 2005 Mar 1;15(5):1497-500.
- PubMed ID
- 15713415 [ View in PubMed]
- Abstract
A series of dimeric PPAR agonists were designed and tested for PPAR activity in vitro. The SAR showed that dimeric ligands with a common group or full dimeric ligands had retained or even increased PPARgamma potency. The dimeric agonist concept can be used to fine tune the subtype selectivity of PPAR agonists. The PPARgamma potency could, at least partly, be explained using molecular modeling.
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 alpha EC 50 (nM) 200 N/A N/A Details