ABSTRACT
U nderstanding the molecular mechanism o f the leptindeptin receptor (OB-R) interaction and the OB-R activation process is crucial for the development o f drugs that target OB-Rs. Recently developed resonance energy transfer (RET)-based assays participated significandy in the establishment o f the current model o f OB-R activation. According to this model, OB-Rs exist as preformed homodimers in the basal state. Leptin binding induces a ligand-induced conformational change within these dimers, which triggers receptor activation by facilitating the transphosphorylation o f receptor-associated janus kinase 2 . The concomitant formation o f tetrameric complexes (dimers o f dimers) has also been suggested but still remains to be firmly established. RET-based techniques also hold great potential for the screening o f small molecular weight compounds targeting the OB-R.
