Different GH secretagogues (peptide and non-peptide) showed both direct ghrelin receptor agonism AND allosteric modulation (positive or negative) of ghrelin binding, revealing complex receptor pharmacology beyond simple agonism.
Key findingMK-677, hexarelin, and other GH secretagogues demonstrated both direct GHS-R agonism and allosteric modulation of ghrelin binding — some enhancing (po
What the researchers found
MK-677, hexarelin, and other GH secretagogues demonstrated both direct GHS-R agonism and allosteric modulation of ghrelin binding — some enhancing (positive) and others reducing (negative) ghrelin's own receptor interaction, revealing complex biased pharmacology.
Why it matters
Relevant for ghrp, mk-677, receptor-signaling, peptide-design.
How the study worked
in-vitro study on ghrp, mk-677.
What this study cannot tell us
See abstract.
How to read the evidence
moderate evidence.
When this study was published
Published in 2005.
The bigger picture
Advances peptide research with clinical implications.
Questions still open
- Further research needed.
- Clinical translation to evaluate.
Common questions
What was studied?
What was found?
Read the original research
Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrelin signaling.
Molecular endocrinology (Baltimore, Md.), 19(9), 2400-11
Citation
Holst, Birgitte; Brandt, Erik; Bach, Anders; Heding, Anders; Schwartz, Thue W. (2005). Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrelin signaling.. Molecular endocrinology (Baltimore, Md.), 19(9), 2400-11.