An odorant derivative as an antagonist for an olfactory receptor
An odorant derivative as an antagonist for an olfactory receptor
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DOI：
10.1093/chemse/bjh247
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发表时间：
2004-11-01
期刊：
影响因子：
3.5
通讯作者：
Touhara, K
中科院分区：
文献类型：
--
作者：
Oka, Y;Nakamura, A;Touhara, K
不同的气味是通过G蛋白偶联嗅觉受体的不同组合来识别的，因此，气味识别是由每种气味的组合受体代码决定的。我们最近证明，气味剂似乎竞争受体位置作为激动剂或拮抗剂。因此，在自然环境中，我们总是感知到各种气味的混合物，气味之间的嗅觉受体拮抗可能导致混合物的受体代码无法从其单个成分的代码中预测。在这里，我们发现储存的异丁香酚对小鼠嗅觉受体有拮抗作用。然而，新鲜纯化的异丁香酚没有抑制作用。相反，在储存过程中产生的异丁香酚衍生物被证明是一种有效的竞争性的mir - eg拮抗剂。结构分析表明，该衍生物是氧化二聚异丁香酚，由氧化反应自然产生。目前的研究表明，随着气味剂的老化，它们会分解或与其他气味剂发生反应，从而影响嗅觉受体的反应性。
Different odorants are recognized by different combinations of G protein-coupled olfactory receptors, and thereby, odor identity is determined by a combinatorial receptor code for each odorant. We recently demonstrated that odorants appeared to compete for receptor sites to act as an agonist or an antagonist. Therefore, in natural circumstances where we always perceive a mixture of various odorants, olfactory receptor antagonism between odorants may result in a receptor code for the mixture that cannot be predicted from the codes for its individual components. Here we show that stored isoeugenol has an antagonistic effect on a mouse olfactory receptor, mOR-EG. However, freshly purified isoeugenol did not have an inhibitory effect. Instead, an isoeugenol derivative produced during storage turned out to be a potent competitive antagonist of mOR-EG. Structural analysis revealed that this derivative is an oxidatively dimerized isoeugenol that naturally occurs by oxidative reaction. The current study indicates that as odorants age, they decompose or react with other odorants, which in turn affects responsiveness of an olfactory receptor(s).