Discovery of a β-MSH-Derived MC-4R Selective Agonist

Autor: Mayer, J. P., Hsiung, H. M., Flora, D. B., Edwards, P., Smith, D. P., Zhang, X.-Y., Gadski, R. A., Heiman, M. L., Hertel, J. L., Emmerson, P. J., Husain, S., O'Brien, T. P., Kahl, S. D., Smiley, D. L., Zhang, L., DiMarchi, R. D., Yan, L. Z.
Zdroj: Journal of Medicinal Chemistry; May 2005, Vol. 48 Issue: 9 p3095-3098, 4p
Abstrakt: 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.
Databáze: Supplemental Index