Further optimization of trisubstituted triazole ghrelin receptor ligands produced compounds with enhanced potency and selectivity, advancing this novel chemical scaffold toward clinical development.
Key findingSecond-generation trisubstituted triazole GHS-R ligands showed improved binding affinity, functional potency, and GH release in vivo compared to first
What the researchers found
Second-generation trisubstituted triazole GHS-R ligands showed improved binding affinity, functional potency, and GH release in vivo compared to first-generation compounds — continued optimization of this novel non-peptide chemical class for GH secretagogue 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
Toward potent ghrelin receptor ligands based on trisubstituted 1,2,4-triazole structure. 2. Synthesis and pharmacological in vitro and in vivo evaluations.
Journal of medicinal chemistry, 50(23), 5790-806
Citation
Moulin, Aline; Demange, Luc; Bergé, Gilbert; Gagne, Didier; Ryan, Joanne; Mousseaux, Delphine; Heitz, Annie; Perrissoud, Daniel; Locatelli, Vittorio; Torsello, Antonio; Galleyrand, Jean-Claude; Fehrentz, Jean-Alain; Martinez, Jean. (2007). Toward potent ghrelin receptor ligands based on trisubstituted 1,2,4-triazole structure. 2. Synthesis and pharmacological in vitro and in vivo evaluations.. Journal of medicinal chemistry, 50(23), 5790-806.