Label-free electrochemical biosensing of small-molecule inhibition on O-GlcNAc glycosylation

CORC > 生态环境研究中心 > 中国科学院生态环境研究中心 > 环境化学与生态毒理学国家重点实验室

	Label-free electrochemical biosensing of small-molecule inhibition on O-GlcNAc glycosylation
	Gu, Yuxin; Guo, Liang-Hong; Yang, Yu; Ren, Xiaomin; Wan, Bin
刊名	BIOSENSORS & BIOELECTRONICS
	2017-12-05
卷号	95 期号:0 页码:94-99
关键词	Electrochemical Tyrosine O-gicnac Glycosylation Inhibition Indium Tin Oxide
英文摘要	O-linked N-acetylglucosamine (O-GlcNAc) transferase (OGT) plays a critical role in modulating protein function in many cellular processes and human diseases such as Alzheimer's disease and type II diabetes, and has emerged as a promising new target. Specific inhibitors of OGT could be valuable tools to probe the biological functions of O-GlcNAcylation, but a lack of robust nonradiometric assay strategies to detect glycosylation, has impeded efforts to identify such compounds. Here we have developed a novel label-free electrochemical biosensor for the detection of peptide O-GleNAcylation using protease-protection strategy and electrocatalytic oxidation of tyrosine mediated by osmium bipyridine as a signal reporter. There is a large difference in the abilities of proteolysis of the glycosylated and the unglycosylated peptides by protease, thus providing a sensing mechanism for OGT activity. When the O-GlcNAcylation is achieved, the glycosylated peptides cannot be cleaved by proteinase K and result in a high current response on indium tin oxide (ITO) electrode. However, when the O-GlcNAcylation is successfully inhibited using a small molecule, the unglycosylated peptides can be cleaved easily and lead to low current signal. Peptide O-GlcNAcylation reaction was performed in the presence of a well-defined small-molecule OGT inhibitor. The results indicated that the biosensor could be used to screen the OGT inhibitors effectively. Our label-free electrochemical method is a promising candidate for protein glycosylation pathway research in screening small-molecule inhibitors of OGT.
内容类型	期刊论文
源URL	[http://ir.rcees.ac.cn/handle/311016/39349]
专题	生态环境研究中心_环境化学与生态毒理学国家重点实验室
推荐引用方式 GB/T 7714	Gu, Yuxin,Guo, Liang-Hong,Yang, Yu,et al. Label-free electrochemical biosensing of small-molecule inhibition on O-GlcNAc glycosylation[J]. BIOSENSORS & BIOELECTRONICS,2017,95(0):94-99.
APA	Gu, Yuxin,Guo, Liang-Hong,Yang, Yu,Ren, Xiaomin,&Wan, Bin.(2017).Label-free electrochemical biosensing of small-molecule inhibition on O-GlcNAc glycosylation.BIOSENSORS & BIOELECTRONICS,95(0),94-99.
MLA	Gu, Yuxin,et al."Label-free electrochemical biosensing of small-molecule inhibition on O-GlcNAc glycosylation".BIOSENSORS & BIOELECTRONICS 95.0(2017):94-99.