CHARACTERIZATION OF A SYNTHETIC TRITIUM-LABELED PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR (HPPAR-GAMMA) LIGAND

[H-3]BRL-49653 was synthesized from its penultimate precursor, dehydro BRL-49653 by tritium gas reduction over a paladium catalyst; specific activity 32 Ci/mmol. Ligand binding studies confirm that [H-3]BRL-496 53 binds with high affinity to human PPAR-gamma. Binding of the recept or-ligand complex to DNA is specific for the appropriate response elem ent and requires heterodimer formation. In this study, RXR's are shown to promote the interaction of PPAR-gamma ligand complex to DNA.