痛苦
黑素皮质素4受体
黑素皮质素
兴奋剂
减肥
肥胖
食物摄入量
黑素皮质素3受体
受体
体重
生物
内分泌学
内科学
医学
药理学
G蛋白偶联受体
黑素皮质激素受体
皮下脂肪
部分激动剂
生物信息学
体重增加
食欲
作者
Jillian L. Seiler,Anna C. Impastato,Emma Xiaoyu Zhang,Kade J Kelley,Thomas L. Bennett,Bradley Studnitzer,Claudia R. Prindle,Benjamin H. Rajewski,Barry A. Badeau,Xinjian Jiang,Russell Potterfield,Jordan Y Delev,Daniel L. Marks
标识
DOI:10.1038/s41467-026-73372-x
摘要
The melanocortin system plays a central role in regulating hunger and satiety, making it an attractive target for treating metabolic disease. However, the limited clinical success of selective melanocortin-4 receptor (MC4R) agonists has prompted investigation into whether concurrent melanocortin-3 receptor (MC3R) and MC4R activation may more effectively engage this pathway for the treatment of general obesity. Here we show that selective MC3R agonism modulates food intake in a state-dependent manner, and that co-agonism of MC3R and MC4R produces greater metabolic effects than selective MC4R agonism alone, consistent with non-redundant and cooperative roles. Using novel peptides in male nonhuman primates and rodents, we develop 710GO, an orally available MC3R/MC4R dual agonist that induces significant weight loss in primates with diet-induced obesity. Oral 710GO demonstrates limited weight rebound, compatibility with GLP-1-based therapies, and a favorable preclinical safety profile. These findings support combined MC3R/MC4R agonism as a promising approach for next-generation obesity therapeutics.
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