Multiple interaction modes between saccharin and sweet taste receptors determine a species-dependent response to saccharin.
Multiple interaction modes between saccharin and sweet taste receptors determine a species-dependent response to saccharin.
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DOI：
10.1002/2211-5463.13355
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发表时间：
2022-03
期刊：
影响因子：
2.6
通讯作者：
Liu B
中科院分区：
文献类型：
--
作者：
Zhao X;Liu M;Cui M;Liu B
甜菊素是一种常用的人工甜味剂，具有增甜和甜味抑制活性。对糖精的物种依赖性反应以及糖精与甜味受体T1 R2/T1 R3之间的相互作用仍然难以捉摸。在这项研究中，我们使用T1 R2和T1 R3的错配嵌合体和钙动员功能分析来揭示人类、松鼠猴和小鼠甜味受体对糖精的详细物种依赖性反应。我们的研究结果，结合以前的结果由他人，表明糖精和甜味受体之间的多种和复杂的相互作用模式，这是有用的指导方针，有效地调制甜味剂/甜味抑制剂。甜菊素具有甜味和甜味抑制活性。除了T1 R2中的正构结合位点激活人甜味受体T1 R2/T1 R3外，T1 R2和T1 R3中似乎还存在至少两个分别抑制受体活性的变构抑制位点，表明糖精与异二聚体甜味受体T1 R2/T1 R3之间存在多种复杂的相互作用模式。
Saccharin is a commonly used artificial sweetener that exhibits both sweetening and sweet inhibition activities. The species‐dependent response towards saccharin and the interaction between saccharin and the sweet taste receptor T1R2/T1R3 remain elusive. In this study we used mismatched chimeras of T1R2 and T1R3 and calcium mobilization functional analysis to reveal a detailed species‐dependent response towards saccharin of human, squirrel monkey, and mouse sweet taste receptors. Our findings, combined with previous results by others, suggest multiple and complex interaction modes between saccharin and the sweet taste receptor, which are helpful guidelines for effective modulation of the sweet taste by sweetener/sweet inhibitors. Saccharin exhibits both sweetening and sweet inhibition activities. Besides the orthosteric binding site in T1R2 for activating the human sweet taste receptor T1R2/T1R3, it appears that there are at least two allosteric inhibitory sites located in T1R2 and T1R3 respectively to inhibit the receptor activity, suggesting multiple and complex interaction modes between saccharin and the heterodimeric sweet taste receptor T1R2/T1R3.
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影响因子：
64.8
作者：
Galindo-Cuspinera, V;Winnig, M;Breslin, PAS
通讯作者：
Breslin, PAS
影响因子：
2.9
作者：
Cheron, Jean-Baptiste;Golebiowski, Jerome;Fiorucci, Sebastien
通讯作者：
Fiorucci, Sebastien
影响因子：
3.1
作者：
Zhao, Meng;Xu, Xiang-Qun;Liu, Bo
通讯作者：
Liu, Bo
DOI：
10.1523/jneurosci.0791-11.2011
发表时间：
2011-07-27
期刊：
The Journal of neuroscience : the official journal of the Society for Neuroscience
影响因子：
--
作者：
Liu B;Ha M;Meng XY;Kaur T;Khaleduzzaman M;Zhang Z;Jiang P;Li X;Cui M
通讯作者：
Cui M
影响因子：
14.9
作者：
THOMPSON, JD;HIGGINS, DG;GIBSON, TJ
通讯作者：
GIBSON, TJ