期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 10, 期 5, 页码 800-805出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.9b00051
关键词
Positive allosteric modulators; Class C GPCR; T1R2/T1R3 receptor; Unnatural peptide; Sweetness enhancer
资金
- Ajinomoto Co., Inc.
T1R2/T1R3 belongs to G protein coupled receptors, which recognizes diverse natural and synthetic sweeteners. A novel class of positive allosteric modulators (PAMs) of T1R2/T1R3 was identified through high-throughput screening campaign. Comparing the structure of the potent compound with previously known PAM, we classified the structure of known PAM into three parts, defined as head, linker, and tail. We then investigated the linker tail structure. It was suggested by molecular docking models of T1R2/T1R3 that an amine that we introduced in the tail was the key for interaction with the receptor binding pocket. We thus synthesized various molecules and found unnatural tripeptide-PAMs, which potently enhance the sweetness of sucrose in sensory evaluation tests.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据