Chapter category:

Study of Leptin: Leptin Receptor Interaction by FRET and BRET

This chapter appears in the following book:

Leptin and Leptin Antagonists

Edited by: Arieh Gertler
ISBN: TBA
» Get more information about this book at landesbioscience.com «

Chapter authors:
Julie Dam, Cyril Couturier, Patty Chen and Ralf Jockers

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Understanding the molecular mechanism of the leptin:leptin receptor (OB‑R) interaction and the OB‑R activation process is crucial for the development of drugs that target OB‑Rs. Recently developed resonance energy transfer (RET)‑based assays participated significantly in the establishment of the current model of 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 of receptor‑associated janus kinase 2. The concomitant formation of tetrameric complexes (dimers of dimers) has also been suggested but still remains to be firmly established. RET‑based techniques also hold great potential for the screening of small molecular weight compounds targeting the OB‑R.

Julie Dam

Cyril Couturier

Patty Chen

Ralf Jockers
Institut Cochin, Université Paris Descartes, CNRS Department of Cell Biology, Paris, France

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Chapter category:

Study of Leptin: Leptin Receptor Interaction by FRET and BRET

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