Microwave-assisted synthesis produced novel macrocyclic peptides active at melanocortin MC1R/MC4R receptors, advancing circular peptide drug design for sexual dysfunction, tanning, and anti-inflammatory applications.
Key findingNovel macrocyclic melanocortin peptides synthesized by microwave-assisted methods showed potent MC1R/MC4R activity, with the macrocyclic constraint im
What the researchers found
Novel macrocyclic melanocortin peptides synthesized by microwave-assisted methods showed potent MC1R/MC4R activity, with the macrocyclic constraint improving receptor selectivity and metabolic stability — advancing circular peptide drugs for melanocortin receptor-mediated therapies.
Why it matters
Relevant for melanotan, pt-141, peptide-design.
How the study worked
in-vitro study.
What this study cannot tell us
See abstract.
How to read the evidence
preliminary evidence.
When this study was published
Published in 2008.
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
Design and microwave-assisted synthesis of novel macrocyclic peptides active at melanocortin receptors: discovery of potent and selective hMC5R receptor antagonists.
Journal of medicinal chemistry, 51(9), 2701-7
Citation
Grieco, Paolo; Cai, Minying; Liu, Lu; Mayorov, Alexander; Chandler, Kevin; Trivedi, Dev; Lin, Guangxin; Campiglia, Pietro; Novellino, Ettore; Hruby, Victor J. (2008). Design and microwave-assisted synthesis of novel macrocyclic peptides active at melanocortin receptors: discovery of potent and selective hMC5R receptor antagonists.. Journal of medicinal chemistry, 51(9), 2701-7. https://doi.org/10.1021/jm701181n