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

Michelle Camerino, Mengjie Liu, Shogo Moriya, Takashi Kitahashi, A. Mahgoub, Simon Mountford, D. K. Chalmers, Tomoko Soga, Ishwar Parhar, Philip Thompson

Research output: Contribution to journalArticleResearchpeer-review

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.
Original languageEnglish
Pages (from-to)406-414
Number of pages9
JournalJournal of Peptide Science
Volume22
Issue number6
DOIs
Publication statusPublished - 1 Jun 2016

Keywords

  • beta amino acids
  • fluorescent peptides
  • KISS1R agonist
  • kisspeptin

Cite this

Camerino, Michelle ; Liu, Mengjie ; Moriya, Shogo ; Kitahashi, Takashi ; Mahgoub, A. ; Mountford, Simon ; Chalmers, D. K. ; Soga, Tomoko ; Parhar, Ishwar ; Thompson, Philip. / Beta amino acid-modified and fluorescently labelled kisspeptin analogues with potent KISS1R activity. In: Journal of Peptide Science. 2016 ; Vol. 22, No. 6. pp. 406-414.
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Beta amino acid-modified and fluorescently labelled kisspeptin analogues with potent KISS1R activity. / Camerino, Michelle; Liu, Mengjie; Moriya, Shogo; Kitahashi, Takashi; Mahgoub, A.; Mountford, Simon; Chalmers, D. K.; Soga, Tomoko; Parhar, Ishwar; Thompson, Philip.

In: Journal of Peptide Science, Vol. 22, No. 6, 01.06.2016, p. 406-414.

Research output: Contribution to journalArticleResearchpeer-review

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AU - Liu, Mengjie

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AU - Kitahashi, Takashi

AU - Mahgoub, A.

AU - Mountford, Simon

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