title: Characterization of the receptor binding residues of kisspeptins by positional scanning using peptide photoaffinity probes.
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.
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto 606-8501, Japan.
authors.forename: Ryosuke
authors.initials: R
authors.lastname: Misu
authors.forename: Shinya
authors.initials: S
authors.lastname: Oishi
authors.forename: Shohei
authors.initials: S
authors.lastname: Setsuda
authors.forename: Taro
authors.initials: T
authors.lastname: Noguchi
authors.forename: Masato
authors.initials: M
authors.lastname: Kaneda
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Ohno
authors.forename: Barry
authors.initials: B
authors.lastname: Evans
authors.forename: Jean-Marc
authors.initials: JM
authors.lastname: Navenot
authors.forename: Stephen C
authors.initials: SC
authors.lastname: Peiper
authors.forename: Nobutaka
authors.initials: N
authors.lastname: Fujii
mesh_terms: D000345:Affinity Labels / Q000737:chemistry*; D000595:Amino Acid Sequence; D001710:Biotin / Q000737:chemistry; D007987:Gonadotropin-Releasing Hormone / Q000378:metabolism; D057809:HEK293 Cells; D006801:Humans; D059648:Kisspeptins / Q000819:agonists* / Q000378:metabolism; D008969:Molecular Sequence Data; D010455:Peptides / Q000737:chemistry* / Q000378:metabolism; D011485:Protein Binding; D018013:Receptors, Neuropeptide / Q000737:chemistry / Q000378:metabolism; D013329:Structure-Activity Relationship; D014466:Ultraviolet Rays
chemical_list: D000345:Affinity Labels; D059648:Kisspeptins; D010455:Peptides; D018013:Receptors, Neuropeptide; D007987:Gonadotropin-Releasing Hormone; D001710:Biotin