Triazole-based small molecules were designed and evaluated as ghrelin receptor ligands, with some showing nanomolar binding and functional activity — expanding the chemical diversity of GH secretagogue drug candidates.
Key findingNovel triazole derivatives showed nanomolar GHS-R1a binding and functional agonist activity in vitro and GH release in vivo, expanding the structural
What the researchers found
Novel triazole derivatives showed nanomolar GHS-R1a binding and functional agonist activity in vitro and GH release in vivo, expanding the structural diversity of non-peptide ghrelin receptor ligands for drug development.
Why it matters
Relevant for ghrp, peptide-design, receptor-signaling.
How the study worked
in-vitro study on ghrp, peptide-design.
What this study cannot tell us
See abstract.
How to read the evidence
preliminary evidence.
When this study was published
Published in 2007.
The bigger picture
Advances peptide research.
Questions still open
- Further research needed.
- Clinical translation to evaluate.
Common questions
What was studied?
What was found?
Read the original research
Synthesis and pharmacological in vitro and in vivo evaluations of novel triazole derivatives as ligands of the ghrelin receptor. 1.
Journal of medicinal chemistry, 50(8), 1939-57
Citation
Demange, Luc; Boeglin, Damien; Moulin, Aline; Mousseaux, Delphine; Ryan, Joanne; Bergé, Gilbert; Gagne, Didier; Heitz, Annie; Perrissoud, Daniel; Locatelli, Vittorio; Torsello, Antonio; Galleyrand, Jean-Claude; Fehrentz, Jean-Alain; Martinez, Jean. (2007). Synthesis and pharmacological in vitro and in vivo evaluations of novel triazole derivatives as ligands of the ghrelin receptor. 1.. Journal of medicinal chemistry, 50(8), 1939-57.