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Development of Dipeptidic hGPR54 Agonists.

Christelle Doebelin1, Isabelle Bertin2, Séverine Schneider1

  • 1Faculté de pharmacie, UMR7200, CNRS, University of Strasbourg, 74 route du Rhin, 67400, Illkirch, France.

Chemmedchem
|August 27, 2016
PubMed
Summary

Researchers developed novel dipeptides targeting the human KiSS1-derived peptide receptor (hGPR54). The compound Bz-Arg-Trp-NH2 demonstrated potent agonistic properties and enhanced stability, significantly increasing testosterone levels in male rats.

Keywords:
GPR54Sonogashira cross-couplingagonistssolid-phase peptide synthesistestosterone

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Area of Science:

  • Medicinal Chemistry
  • Neuroendocrinology
  • Peptide Synthesis

Background:

  • The human KiSS1-derived peptide receptor (hGPR54) plays a crucial role in reproductive functions.
  • Endogenous ligands like kisspeptin are susceptible to rapid degradation, limiting their therapeutic potential.

Purpose of the Study:

  • To design and synthesize novel dipeptide agonists of hGPR54.
  • To enhance the stability and in vivo efficacy of hGPR54 agonists.

Main Methods:

  • Convergent solid-phase peptide synthesis utilizing Sonogashira cross-coupling reactions.
  • Affinity and functional assays to evaluate receptor binding and agonistic activity.
  • In vitro stability assays (serum, liver microsomes) and in vivo studies in male rats.

Main Results:

  • A series of N-terminally modified dipeptides were synthesized, exhibiting sub-micromolar affinities for hGPR54.
  • The benzoylated dipeptide Bz-Arg-Trp-NH2 emerged as the most potent agonist.
  • Bz-Arg-Trp-NH2 displayed significantly improved stability compared to kisspeptin and induced a notable increase in testosterone levels in vivo.

Conclusions:

  • Novel, stable dipeptide agonists of hGPR54 were successfully developed.
  • Bz-Arg-Trp-NH2 represents a promising therapeutic candidate for conditions related to hGPR54 signaling.
  • The synthetic strategy allows for further optimization of hGPR54-targeting compounds.