Structure–CaSR–Activity Relation of <i>Kokumi</i> γ-Glutamyl Peptides
作者:Yusuke Amino、Masakazu Nakazawa、Megumi Kaneko、Takashi Miyaki、Naohiro Miyamura、Yutaka Maruyama、Yuzuru Eto
DOI:10.1248/cpb.c16-00293
日期:——
activities have been shown to be positively correlated, suggesting that kokumi gamma-glutamyl peptides are perceived through CaSRs in humans. Our research is based on the hypothesis that the discovery of highly active CaSR agonist peptides will lead to the creation of practical kokumi peptides. Through continuous study of the structure-CaSR-activity relation of a large number of gamma-glutamyl peptides, we have
钙敏感受体(CaSR)的调节是诸如谷胱甘肽(gamma-glutamylcysteinylglycine)等gamma-谷氨酰肽的生理活性之一。γ-谷氨酰肽还具有增香作用,即浓香物质的感官活性,当添加到食品中时,可以改变五种基本口味。这些活性已经显示出正相关,这表明通过人的CaSR可以感知到kokumiγ-谷氨酰胺肽。我们的研究基于以下假设:高活性CaSR激动剂肽的发现将导致创建实用的kokumi肽。通过不断研究大量γ-谷氨酰胺肽的结构-CaSR-活性关系,我们已经确定了强烈的γ-谷氨酰肽的CaSR活性的结构要求如下:-存在N-末端γ-L-谷氨酰基残基;在L-构型的第二个残基处存在中等大小的脂族中性取代基;存在C端羧酸,优选存在甘氨酸作为第三组分。通过使用CaSR活性测定法筛选而选出的γ-谷氨酰肽的感官分析,发现γ-谷氨酰戊基甘氨酸是强效的kokumi肽。此外,含降冰片碱的γ-谷氨酰肽,即