Abstract
We report the development of macrocyclic melanocortin derivatives of MT-II and SHU-9119, achieved by modifying the cycle dimension and incorporating constrained amino acids in ring-closing. This study culminated in the discovery of novel agonists/antagonists with an unprecedented activity profile by adding pieces to the puzzle of the melanocortin receptor selectivity. Finally, the resulting 19- and 20-membered rings represent a suitable frame for the design of further therapeutic ligands as selective modulators of the melanocortin system.
Original language | English (US) |
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Pages (from-to) | 4263-4269 |
Number of pages | 7 |
Journal | Journal of Medicinal Chemistry |
Volume | 61 |
Issue number | 9 |
DOIs | |
State | Published - May 10 2018 |
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery