Activation of Neuropeptide FF Receptors by Kisspeptin Receptor Ligands
| Autor: | Hiroaki Ohno, Gozoh Tsujimoto, Nahoko Ieda, Hiroko Tsukamura, Kenji Tomita, Ryosuke Misu, Satoshi Ohkura, Naoko Inoue, Shinya Oishi, Akira Hirasawa, Kei-ichiro Maeda, Yoshihisa Uenoyama, Ryo Masuda, Nobutaka Fujii, Shohei Setsuda, Yousuke Naniwa |
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| Jazyk: | angličtina |
| Rok vydání: | 2010 |
| Předmět: |
Agonist
medicine.medical_specialty medicine.drug_class Organic Chemistry Neuropeptide Neuropeptide FF receptor Biology Biochemistry Gonadotropin secretion Endocrinology Kisspeptin Internal medicine Drug Discovery medicine Neuropeptide FF Receptor hormones hormone substitutes and hormone antagonists G protein-coupled receptor |
| Popis: | Kisspeptin is a member of the RFamide neuropeptide family that is implicated in gonadotropin secretion. Because kisspeptin-GPR54 signaling is implicated in the neuroendocrine regulation of reproduction, GPR54 ligands represent promising therapeutic agents against endocrine secretion disorders. In the present study, the selectivity profiles of GPR54 agonist peptides were investigated for several GPCRs, including RFamide receptors. Kisspeptin-10 exhibited potent binding and activation of neuropeptide FF receptors (NPFFR1 and NPFFR2). In contrast, short peptide agonists bound with much lower affinity to NPFFRs while showing relatively high selectivity toward GPR54. The possible localization of secondary kisspeptin targets was also demonstrated by variation in the levels of GnRH release from the median eminence and the type of GPR54 agonists used. Negligible affinity of the reported NPFFR ligands to GPR54 was observed and indicates the unidirectional cross-reactivity between both ligands. |
| Databáze: | OpenAIRE |
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