Characterization of the receptor binding residues of kisspeptins by positional scanning using peptide photoaffinity probes |
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Authors: | Ryosuke Misu Shinya Oishi Shohei Setsuda Taro Noguchi Masato Kaneda Hiroaki Ohno Barry Evans Jean-Marc Navenot Stephen C. Peiper Nobutaka Fujii |
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Affiliation: | 1. Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan;2. Department of Pathology, Anatomy and Cell Biology, Thomas Jefferson University, Philadelphia, PA 19107, USA |
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Abstract: | Kisspeptins, endogenous peptide ligands for GPR54, play an important role in GnRH secretion. Since in vivo administration of kisspeptins induces increased plasma LH levels, GPR54 agonists hold promise as therapeutic agents for the treatment of hormonal secretion diseases. To facilitate the design of novel potent GPR54 ligands, residues in kisspeptins that involve in the interaction with GPR54 were investigated by kisspeptin-based photoaffinity probes. Herein, we report the design and synthesis of novel kisspeptin-based photoaffinity probes, and the application to crosslinking experiments for GPR54-expressing cells. |
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