Behrens Maik, Brockhoff Anne, Kuhn Christina, Bufe Bernd, Winnig Marcel, Meyerhof Wolfgang
Department of Molecular Genetics, German Institute of Human Nutrition, Potsdam-Rehbruecke, Arthur-Scheunert-Allee 114-116, 14558 Nuthetal, Germany.
Biochem Biophys Res Commun. 2004 Jun 25;319(2):479-85. doi: 10.1016/j.bbrc.2004.05.019.
The recent advances in the functional expression of TAS2Rs in heterologous systems resulted in the identification of bitter tastants that specifically activate receptors of this family. All bitter taste receptors reported to date exhibit a pronounced selectivity for single substances or structurally related bitter compounds. In the present study we demonstrate the expression of the hTAS2R14 gene by RT-PCR analyses and in situ hybridisation in human circumvallate papillae. By functional expression in HEK-293T cells we show that hTAS2R14 displays a, so far, unique broad tuning towards a variety of structurally diverse bitter compounds, including the potent neurotoxins, (-)-alpha-thujone, the pharmacologically active component of absinthe, and picrotoxinin, a poisonous substance of fishberries. The observed activation of heterologously expressed hTAS2R14 by low concentrations of (-)-alpha-thujone and picrotoxinin suggests that the receptor is sufficiently sensitive to caution us against the ingestion of toxic amounts of these substances.
TAS2Rs在异源系统中的功能表达方面的最新进展,使得能够鉴定出特异性激活该家族受体的苦味剂。迄今为止报道的所有苦味受体对单一物质或结构相关的苦味化合物都表现出明显的选择性。在本研究中,我们通过RT-PCR分析和原位杂交证明了hTAS2R14基因在人轮廓乳头中的表达。通过在HEK-293T细胞中的功能表达,我们表明hTAS2R14对多种结构多样的苦味化合物表现出一种迄今为止独特的广泛调谐,包括强效神经毒素(-)-α-侧柏酮(苦艾酒的药理活性成分)和印防己毒素(鱼藤莓的一种有毒物质)。观察到低浓度的(-)-α-侧柏酮和印防己毒素对异源表达的hTAS2R14的激活表明,该受体足够敏感,提醒我们要警惕摄入这些物质的有毒量。