Discovery of a β-MSH-Derived MC-4R Selective Agonist
- 12 April 2005
- journal article
- letter
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 48 (9) , 3095-3098
- https://doi.org/10.1021/jm0501432
Abstract
A series of novel, disulfide-constrained human β-melanocyte stimulating hormone (β-MSH)-derived peptides were optimized for in vitro melanocortin-4 receptor (MC-4R) binding affinity, agonist efficacy, and selectivity. The most promising of these, analogue 18, was further studied in vivo using chronic rat food intake and body weight models.Keywords
This publication has 18 references indexed in Scilit:
- Feeding and behavioural effects of central administration of the melanocortin 3/4-R antagonist SHU9119 in obese and lean Siberian hamstersBehavioural Brain Research, 2004
- The Epidemic of ObesityJournal of Clinical Endocrinology & Metabolism, 2004
- Melanocortin receptors weigh inNature Medicine, 2004
- Melanocortin ligands: 30 years of structure–activity relationship (SAR) studiesMedicinal Research Reviews, 2004
- Selective, High Affinity Peptide Antagonists of α-Melanotropin Action at Human Melanocortin Receptor 4: Their Synthesis and Biological Evaluation in VitroJournal of Medicinal Chemistry, 2001
- Inefficient gene transfer by adenovirus vector to cystic fibrosis airway epithelia of mice and humansNature, 1994
- The Cloning of a Family of Genes That Encode the Melanocortin ReceptorsScience, 1992
- [half-Cys4,half-Cys10]-alpha-Melanocyte-stimulating hormone: a cyclic alpha-melanotropin exhibiting superagonist biological activity.Proceedings of the National Academy of Sciences, 1982
- 4-Norleucine, 7-D-phenylalanine-alpha-melanocyte-stimulating hormone: a highly potent alpha-melanotropin with ultralong biological activity.Proceedings of the National Academy of Sciences, 1980
- Evidence for two separate opiate peptide neuronal systemsNature, 1978