The G-protein coupling properties of the human sweet and amino acid taste receptors.
The G-protein coupling properties of the human sweet and amino acid taste receptors.
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人类甜味和氨基酸味觉受体的 G 蛋白偶联特性。
DOI：
10.1002/dneu.20403
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发表时间：
2007
影响因子：
3
通讯作者：
Sullivan,SusanL
中科院分区：
文献类型：
--
作者：
Sainz,Eduardo;Cavenagh,MargaretM;LopezJimenez,NelsonD;Gutierrez,JoanneC;Battey,JamesF;Northup,JohnK;Sullivan,SusanL
人类T1 R味觉受体是家族C G蛋白偶联受体（GPCR），其作为异二聚体介导甜味（hT 1 R2 + hT 1 R3）和鲜味（hT 1 R1 + hT 1 R3）味觉模式。每个T1 R都有一个大的细胞外配体结合结构域，连接到一个七跨膜核心结构域（7 TMD）。我们证明hT 1 R1和hT 1 R2的7 TMD显示出强大的配体非依赖性组成活性，有效催化Gα亚基上GDP与GTP的交换。相比之下，相对于hT 1 R1和hT 1 R2的7 TMD，hT 1 R3的7 TMD与G蛋白的偶联较差，这表明体内信号传导可能主要通过hT 1 R1和hT 1 R2进行。此外，我们还提供了直接证据，证明hT 1受体选择性地通过Gαi/o途径，与多个Gαi/o亚基以及味觉细胞特异性Gβ1γ 13二聚体偶联。© 2007 Wiley Periodicals，Inc.开发神经生物学，2007年。
The human T1R taste receptors are family C G‐protein‐coupled receptors (GPCRs) that act as heterodimers to mediate sweet (hT1R2 + hT1R3) and umami (hT1R1 + hT1R3) taste modalities. Each T1R has a large extracellular ligand‐binding domain linked to a seven transmembrane‐spanning core domain (7TMD). We demonstrate that the 7TMDs of hT1R1 and hT1R2 display robust ligand‐independent constitutive activity, efficiently catalyzing the exchange of GDP for GTP on Gα subunits. In contrast, relative to the 7TMDs of hT1R1 and hT1R2, the 7TMD of hT1R3 couples poorly to G‐proteins, suggesting thatin vivosignaling may proceed primarily through hT1R1 and hT1R2. In addition, we provide direct evidence that the hT1Rs selectively signal through Gαi/opathways, coupling to multiple Gαi/osubunits as well as the taste cell specific Gβ1γ13dimer. © 2007 Wiley Periodicals, Inc. Develop Neurobiol, 2007.