银杏酸参与α - 1甘氨酸受体正向调节的氨基酸残基。

G. Maleeval, S. Buldakoval, G. Skibo, P. Bregestovski
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引用次数: 1

摘要

先前,我们已经证明银杏酸具有增强电流的能力,由甘氨酸受体α 1亚基介导。为了明确银杏酸亚基特异性作用的机制,我们对甘氨酸受体at和α2亚基的氨基酸序列进行了比较分析。确定了银杏酸对这些亚基形成的甘氨酸受体的不同作用的氨基酸。利用膜片钳记录的全细胞结构,我们证实α2亚基的三个残基突变为α 1亚基的相应残基,使α2受体对银杏酸的增强敏感。α2突变体受体介导的电流在银杏酸处理后增加了89±14%。与ai受体类似,α2突变体受体在EC₅0上也有所下降。对甘氨酸在银杏酸的作用下。因此,银杏酸的亚基选择性与甘氨酸受体α1和α2亚基中不同的三个氨基酸残基密切相关。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
AMINOACID RESIDUES INVOLVED IN POSITIVE MODULATION OF αl GLYCINE RECEPTORS BY GINKGOLIC ACID.
Previously, we have shown that ginkgolic acid has an ability to potentiate currents, mediated by αl subunits of glycine receptor. In order to define the mechanism of subunit specific action of ginkgolic acid we have performed comparative analysis of the amino acid sequences of at and α2 subunits of glycine receptor. Amino acids that contribute to the different action of ginkgolic acid on glycine receptors formed by these subunits were determined. Using whole-cell configuration of patch-clamp recording, we have demonstrated that mutation of three residues in α2 subunit for corresponding ones from αl subunit makes α2 receptors sensitive to the potentiation by ginkgolic acid. Currents, mediated by α2 mutant receptors, increased by 89±14% after application of ginkgolic acid. Similarly to ai receptors α2 mutant receptors have shown a decrease in EC₅₀. for glycine under the action of ginkgolic acid. Thus, subunit selectivity of the ginkgolic acid is in strong connection with three amino acid residues that are different in α1 And α2 subunits of glycine receptor.
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