- Discovery of a beta-MSH-derived MC-4R selective agonist.
Discovery of a beta-MSH-derived MC-4R selective agonist.
Journal of medicinal chemistry (2005-04-29)
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
PMID15857110
摘要
A series of novel, disulfide-constrained human beta-melanocyte stimulating hormone (beta-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.
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