Synthetic GH secretagogues functioned as orthosteric super-agonists (more potent than ghrelin itself) rather than allosteric modulators at the GHS-R1a receptor, clarifying their mechanism as direct receptor activators that exceed the natural ligand.
Key findingPeptidyl and non-peptidyl GH secretagogues acted as orthosteric super-agonists at GHS-R1a (exceeding ghrelin's own maximal receptor activation) rather
What the researchers found
Peptidyl and non-peptidyl GH secretagogues acted as orthosteric super-agonists at GHS-R1a (exceeding ghrelin's own maximal receptor activation) rather than allosteric modulators — they directly activate the receptor more potently than the natural hormone itself.
Why it matters
Relevant for peptide research.
How the study worked
research study.
What this study cannot tell us
See abstract.
How to read the evidence
emerging evidence.
When this study was published
Published in 2009.
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
Growth hormone secretagogues and growth hormone releasing peptides act as orthosteric super-agonists but not allosteric regulators for activation of the G protein Galpha(o1) by the Ghrelin receptor.
Molecular pharmacology, 76(4), 802-11
Citation
Bennett, Kirstie A; Langmead, Christopher J; Wise, Alan; Milligan, Graeme. (2009). Growth hormone secretagogues and growth hormone releasing peptides act as orthosteric super-agonists but not allosteric regulators for activation of the G protein Galpha(o1) by the Ghrelin receptor.. Molecular pharmacology, 76(4), 802-11. https://doi.org/10.1124/mol.109.056101