磷酸化和类香草配体结构在配体依赖性差异激活瞬时受体电位类香草素 1 中的作用。

IF 1.4 4区 生物学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
Sakura Moriyama, Kenji Tatematsu, Shuji Hinuma, Shun'ichi Kuroda
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引用次数: 0

摘要

根据对福斯可林(FSK)的敏感性,可激活瞬时受体电位香草素 1(TRPV1)的香草素类似物被分为两种类型。用 FSK 处理表达 TRPV1 的细胞可增强 TRPV1 对辣椒素类配体的反应,同时降低对丁香酚类配体的反应。在本研究中,我们通过表达 TRPV1 的 HEK293T 细胞中 Ca2+ 的流入,确定了 FSK 对鹅膏类配体刺激 TRPV1 激活的影响。我们的研究结果表明,FSK 的作用可归因于 TRPV1 的磷酸化,使用蛋白激酶 A(PKA)抑制剂和潜在磷酸化位点的 TRPV1 突变体证明了这一点。此外,我们还研究了 13 种香草类似物的结构-活性关系。我们的研究结果表明,类香草素化合物可分为三种类型,即之前报道的两种类型和一种新型的 10-shogaol,通过这两种类型激活的 TRPV1 不受 FSK 处理的影响。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Role of phosphorylation and vanilloid ligand structure in ligand-dependent differential activations of transient receptor potential vanilloid 1.

Vanilloid analogs, which can activate transient receptor potential vanilloid 1 (TRPV1), have been classified into two types based on susceptibility to forskolin (FSK). Treatment of cells expressing TRPV1 with FSK enhances TRPV1 responses to capsaicin-type ligands while diminishing the responses to eugenol-type ligands. In this study, we determined the effect of FSK on the activation of TRPV1 stimulated with vanilloid ligands, through the influx of Ca2+ in HEK293T cells expressing TRPV1. Our findings suggest that the effects of FSK can be attributed to the phosphorylation of TRPV1, as evidenced by using a protein kinase A inhibitor and TRPV1 mutants at potential phosphorylation sites. Furthermore, we examined the structure-activity relationship of 13 vanilloid analogs. Our results indicated that vanilloid compounds could be classified into three types, that is the previously reported two types and a novel type of 10-shogaol, by which TRPV1 activation was insusceptible to the FSK treatment.

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来源期刊
Bioscience, Biotechnology, and Biochemistry
Bioscience, Biotechnology, and Biochemistry 生物-生化与分子生物学
CiteScore
3.50
自引率
0.00%
发文量
183
审稿时长
1 months
期刊介绍: Bioscience, Biotechnology, and Biochemistry publishes high-quality papers providing chemical and biological analyses of vital phenomena exhibited by animals, plants, and microorganisms, the chemical structures and functions of their products, and related matters. The Journal plays a major role in communicating to a global audience outstanding basic and applied research in all fields subsumed by the Japan Society for Bioscience, Biotechnology, and Agrochemistry (JSBBA).
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