Beta amino acid-modified and fluorescently labelled kisspeptin analogues with potent KISS1R activity

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‐transf...

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Bibliographic Details
Published in:Journal of peptide science 2016-06, Vol.22 (6), p.406-414
Main Authors: Camerino, M. A., Liu, M., Moriya, S., Kitahashi, T., Mahgoub, A., Mountford, S. J., Chalmers, D. K., Soga, T., Parhar, I. S., Thompson, P. E.
Format: Article
Language:English
Subjects:
Amino Acids - chemistry
beta amino acids
Fluorescent Dyes - chemistry
fluorescent peptides
HEK293 Cells
Humans
KISS1R agonist
kisspeptin
Kisspeptins - agonists
Ligands
Peptides
Receptors, G-Protein-Coupled - chemistry
Receptors, G-Protein-Coupled - metabolism
Receptors, Kisspeptin-1
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Summary: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. Known and novel kisspeptin analogues were assayed utilising a dual luciferase reporter assay in KISS1R‐transfected HEK293T cells. β2‐hTyr‐modified and fluorescently labelled analogues were identified as potent KISS1R agonists. Proteolysis may diminish the agonist outputs in the reporter assay.
ISSN:1075-2617
1099-1387
DOI:10.1002/psc.2883