Structure-activity relationships of dimeric PPAR agonists.
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.
Sauerberg
Per
P
Novo Nordisk A/S, Novo Nordisk Park, 2760 Måløv, Denmark. psa@novonordisk.com
Mogensen
John P
JP
Jeppesen
Lone
L
Svensson
L Anders
LA
Fleckner
Jan
J
Nehlin
Jan
J
Wulff
Erik M
EM
Pettersson
Ingrid
I
D019281:Dimerization; D015195:Drug Design; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D047492:Peroxisome Proliferator-Activated Receptors / Q000819:agonists* / Q000737:chemistry; D013329:Structure-Activity Relationship
D008024:Ligands; D047492:Peroxisome Proliferator-Activated Receptors