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发明公开
CN108329393A T1R异源寡聚的味觉受体和表达所述受体的细胞系及其在鉴定味觉化合物中的用途 失效 - 放弃专利权 转让

T1R异源寡聚的味觉受体和表达所述受体的细胞系及其在鉴定味觉化合物中的用途
摘要：
本发明涉及T1R受体装配形成功能性味觉受体的发现。具体而言，本发明发现共表达T1R1和T1R3可产生响应鲜味刺激物(包括谷氨酸一钠)的味觉受体。还发现共表达T1R2和T1R3受体可产生响应甜味刺激物(包括天然存在的以及人造的甜味剂)的味觉受体。本发明还涉及包含T1R1/T1R3和T1R2/T1R3的异寡聚味觉受体在分析中的用途，用于鉴定分别响应鲜味刺激物和甜味刺激物的化合物。本发明另外涉及构建在组成型或诱导型条件下稳定或瞬时共表达T1R1和T1R3、或T1R2和T1R3组合的细胞系。本发明还提供了这些细胞系在基于细胞的分析、特别是利用荧光成像检测受体活性的高通量筛选分析中的用途，用于鉴定鲜味和甜味调节剂化合物。最后，本发明涉及以下发现，即某些化合物，例如拉克替醇(lactisole)，抑制人T1R2/T1R3和T1R1/T1R3受体活性，从而抑制甜味和鲜味觉，提示这些受体可能是唯一的甜味和鲜味受体。
摘要（英）：

The present invention relates to the discovery that the T1R receptors assemble to form functional taste receptors. Particularly, it has been discovered that co-expression of T1R1 and T1R3 results in ataste receptor that responds to umami taste stimuli, including monosodium glutamate. Also, it has been discovered that co-expression of the T1R2 and T1R3 receptors results in a taste receptor that responds to sweet taste stimuli including naturally occurring and artificial sweeteners. Also the present invention relates to the use of hetero-oligomeric taste receptors comprising T1R1/T1R3 and T1R2/T1R3 in assays to identify compounds that respectively respond to umami taste stimuli and sweet taste stimuli. Further, the invention relates to the constitutive of cell lines that stably or transiently co-express a combination of T1R1 and T1R3; or T1R2 and T1R3; under constitutive or inducible conditions. The use of these cells lines in cell-based assays to identify umami and sweet taste modulatory compounds is also provided, particularly high throughput screening assays that detect receptor activity by use of fluorometric imaging. Finally, the invention relates to the discovery that some compounds, e.g., lactisole, inhibit both the activities of human T1R2/T1R3 and T1R1/T1R3 receptors, and accordingly the sweet and umami taste, suggesting that these receptors may be the only sweet and umami receptors.

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