Structure-activity relationships of dimeric PPAR agonists.

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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
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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
DrugTargetPropertyMeasurementpHTemperature (°C)
RosiglitazonePeroxisome proliferator-activated receptor alphaEC 50 (nM)4100N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor alphaEC 50 (nM)200N/AN/ADetails