一种源自β-促黑素的促黑素细胞激素4型受体（MC-4R）选择性激动剂的发现。
Discovery of a beta-MSH-derived MC-4R selective agonist.
作者信息
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
机构信息
Lilly Research Laboratories, A Division of Eli Lilly and Co., Lilly Corporate Center, Indianapolis, Indiana 46285, USA.
出版信息
J Med Chem. 2005 May 5;48(9):3095-8. doi: 10.1021/jm0501432.
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.
一系列新型的、具有二硫键约束的人β-促黑素细胞激素（β-MSH）衍生肽针对体外黑素皮质素-4受体（MC-4R）的结合亲和力、激动剂效力和选择性进行了优化。其中最有前景的类似物18，使用慢性大鼠食物摄入量和体重模型在体内进行了进一步研究。
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