Beta amino acid‐modified and fluorescently labelled kisspeptin analogues with potent KISS1R activity |
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| Authors: | M. A. Camerino M. Liu S. Moriya T. Kitahashi A. Mahgoub S. J. Mountford D. K. Chalmers T. Soga I. S. Parhar P. E. Thompson |
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| Affiliation: | 1. Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia;2. Brain Research Institutes, Monash University Malaysia, Selangor, Malaysia |
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| Abstract: | Kisspeptin analogues with improved metabolic stability may represent important ligands in the study of the kisspeptin/KISS1R system and have therapeutic potential. In this paper we assess the activity of known and novel kisspeptin analogues utilising a dual luciferase reporter assay in KISS1R‐transfected HEK293T cells. In general terms the results reflect the outcomes of other assay formats and a number of potent agonists were identified among the analogues, including β2‐hTyr‐modified and fluorescently labelled forms. We also showed, by assaying kisspeptin in the presence of protease inhibitors, that proteolysis of kisspeptin activity within the reporter assay itself may diminish the agonist outputs. Copyright © 2016 European Peptide Society and John Wiley & Sons, Ltd. |
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| Keywords: | kisspeptin KISS1R agonist beta amino acids fluorescent peptides |
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