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Updated: Jan 8, 2026

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SAR研究和setmelanotide的协同优化产生了一种强效,选择性和可溶性MC4R激活剂

Chen Guo1, Tao Luo2, Yuanzhen Dong3

  • 1School of Pharmaceutical Sciences, Shanghai Jiao Tong University, 200240 Shanghai, China; National Key Laboratory of Lead Druggability Research, 201203 Shanghai, China.

Bioorganic chemistry
|December 16, 2025
PubMed
概括

研究人员开发了一种新的,SC19,以改善肥胖治疗中的setmelanotide. SC19显示出增强的溶解性和选择性,提供潜在的治疗益处,副作用较少.

关键词:
黑色皮质素-4受体 (MC4R) 是一种酸的化学结构受体的选择性受体的选择性塞特梅兰诺提德 (Setmelanotide) 是一种一种结构与活动关系 (SAR)

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Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
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