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

Mayer, John P.; Hsiung, Hansen M.; Flora, David B.; Edwards, Patrick; Smith, Dennis P.; Zhang, Xing-Yue; Gadski, Robert A.; Heiman, Mark L.; Hertel, JeAnne L.; Emmerson, Paul J.; Husain, Saba; O'Brien, Thomas P.; Kahl, Steven D.; Smiley, David L.; Zhang, Lianshan; DiMarchi, Richard D.; Yan, Liang Zeng

doi:10.1021/jm0501432.s001

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

https://doi.org/10.1021/jm0501432.s001
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journal contribution

posted on 2005-05-05, 00:00 authored by John P. Mayer, Hansen M. Hsiung, David B. Flora, Patrick Edwards, Dennis P. Smith, Xing-Yue Zhang, Robert A. Gadski, Mark L. Heiman, JeAnne L. Hertel, Paul J. Emmerson, Saba Husain, Thomas P. O'Brien, Steven D. Kahl, David L. Smiley, Lianshan Zhang, Richard D. DiMarchi, Liang Zeng Yan

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.