title: Structure-activity relationships of dimeric PPAR agonists.
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.
authors.affiliation: Novo Nordisk A/S, Novo Nordisk Park, 2760 Måløv, Denmark. psa@novonordisk.com
authors.forename: Per
authors.initials: P
authors.lastname: Sauerberg
authors.forename: John P
authors.initials: JP
authors.lastname: Mogensen
authors.forename: Lone
authors.initials: L
authors.lastname: Jeppesen
authors.forename: L Anders
authors.initials: LA
authors.lastname: Svensson
authors.forename: Jan
authors.initials: J
authors.lastname: Fleckner
authors.forename: Jan
authors.initials: J
authors.lastname: Nehlin
authors.forename: Erik M
authors.initials: EM
authors.lastname: Wulff
authors.forename: Ingrid
authors.initials: I
authors.lastname: Pettersson
mesh_terms: 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
chemical_list: D008024:Ligands; D047492:Peroxisome Proliferator-Activated Receptors