Molecular mechanism of the sweet taste enhancers

Feng Zhang; Boris Klebansky; Richard M. Fine; Haitian Liu; Hong Xu; Guy Servant; Mark Zoller; Catherine Tachdjian; Xiaodong Li

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Molecular mechanism of the sweet taste enhancers

机译：甜味增强剂的分子机理

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摘要

Positive allosteric modulators of the human sweet taste receptor have been developed as a new way of reducing dietary sugar intake. Besides their potential health benefit, the sweet taste enhancers are also valuable tool molecules to study the general mechanism of positive allosteric modulations of T1R taste receptors. Using chimeric receptors, mutagenesis, and molecular modeling, we reveal how these sweet enhancers work at the molecular level. Our data argue that the sweet enhancers follow a similar mechanism as the natural umami taste enhancer molecules. Whereas the sweeteners bind to the hinge region and induce the closure of the Venus flytrap domain of T1R2, the enhancers bind close to the opening and further stabilize the closed and active conformation of the receptor.

机译：已经开发了人类甜味受体的正构构调节剂，作为减少饮食中糖摄入量的新方法。除了潜在的健康益处外，甜味增强剂也是研究T1R味觉受体正变构调节的一般机制的有价值的工具分子。使用嵌合受体，诱变和分子建模，我们揭示了这些甜味增强剂如何在分子水平上发挥作用。我们的数据认为，甜味增强剂遵循与天然鲜味增强剂分子相似的机制。甜味剂与铰链区结合并诱导T1R2的维纳斯捕蝇器结构域关闭，而增强剂则在开口附近结合并进一步稳定受体的闭合和活性构象。

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来源
《Proceedings of the National Academy of Sciences of the United States of America》 |2010年第10期|p.4752-4757|共6页
作者
Feng Zhang; Boris Klebansky; Richard M. Fine; Haitian Liu; Hong Xu; Guy Servant; Mark Zoller; Catherine Tachdjian; Xiaodong Li;
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作者单位

Senomyx, Inc., San Diego, CA 92121;

BioPredict, Inc., Oradell, NJ 07649;

BioPredict, Inc., Oradell, NJ 07649;

Senomyx, Inc., San Diego, CA 92121;

Senomyx, Inc., San Diego, CA 92121;

Senomyx, Inc., San Diego, CA 92121;

Senomyx, Inc., San Diego, CA 92121;

Senomyx, Inc., San Diego, CA 92121;

Senomyx, Inc., San Diego, CA 92121;

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收录信息美国《科学引文索引》(SCI);美国《生物学医学文摘》(MEDLINE);美国《化学文摘》(CA);
原文格式 PDF
正文语种 eng
中图分类
关键词
positive allosteric modulators; sweet taste receptor; T1R;

机译：正变构调节剂;甜味受体;T1R;

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6. Molecular mechanism of the sweet taste enhancers [O] . Feng Zhang, Boris Klebansky, Richard M. Fine, 2010

机译：甜味增强剂的分子机理
7. Molecular mechanism of the sweet taste enhancers [O] . Zhang, Feng, Klebansky, Boris, Fine, Richard M., 2010

机译：甜味增强剂的分子机理

Molecular mechanism of the sweet taste enhancers

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