The structure-based traceless specific fluorescence labeling of the smoothened receptor

doi:10.1039/c9ob00654k

	The structure-based traceless specific fluorescence labeling of the smoothened receptor
	Xue, Dongxiang1,2,3,4 ; Ye, Lintao1 ; Zheng, Jun4 ; Wu, Yiran1 ; Zhang, Xianjun1 ; Xu, Yueming1 ; Li, Tao1 ; Stevens, Raymond C.1,4 ; Xu, Fei1,4 ; Zhuang, Min4 ; Zhao, Suwen1,4 ; Zhao, Fei1 ; Tao, Houchao1
	2019-07-07
发表期刊	ORGANIC & BIOMOLECULAR CHEMISTRY (IF:2.9[JCR-2023],2.8[5-Year])
ISSN	1477-0520
卷号	17 期号:25 页码:6136-6142
发表状态	已发表
DOI	10.1039/c9ob00654k
摘要	The smoothened receptor (SMO) mediates the hedgehog (Hh) signaling pathway and plays a vital role in embryonic development and tumorigenesis. The visualization of SMO has the potential to provide new insights into its enigmatic mechanisms and associated disease pathogenesis. Based on recent progress in structural studies of SMO, we have designed and characterized a group of affinity probes to facilitate the turn-on fluorescence labeling of SMO at the epsilon-amine of K395. These chemical probes were derived from a potent SMO antagonist skeleton by the conjugation of a small non-fluorescent unit, O-nitrobenzoxadiazole (O-NBD). In this context, optimal probes were developed to be capable of efficiently and selectively lighting up SMO regardless of whether it is in micelles or in native membranes. More importantly, the resulting labeled SMO only bears a very small fluorophore and allows for the recovery of the unoccupied pocket by dissociation of the residual ligand module. These advantages should allow the probe to serve as a potential tool for monitoring SMO trafficking, understanding Hh activation mechanisms, and even the diagnosis of tumorigenesis in the future.
收录类别	EI ; SCIE ; SCI ; IC
语种	英语
资助项目	National Natural Science Foundation of China[21672147] ; National Natural Science Foundation of China[21708026]
WOS研究方向	Chemistry
WOS类目	Chemistry, Organic
WOS记录号	WOS:000473052800006
出版者	ROYAL SOC CHEMISTRY
EI入藏号	20192707131075
EI主题词	Diagnosis ; Micelles ; Probes
EI分类号	Medicine and Pharmacology:461.6 ; Light/Optics:741.1 ; Colloid Chemistry:801.3
WOS关键词	HEDGEHOG ; PROTEINS ; BINDING ; LIGANDS ; PROBES
原始文献类型	Article
引用统计	正在获取...
文献类型	期刊论文
条目标识符	https://kms.shanghaitech.edu.cn/handle/2MSLDSTB/57598
专题	生命科学与技术学院_博士生生命科学与技术学院_PI研究组_庄敏组 iHuman研究所_特聘教授组_Raymond Stevens组 iHuman研究所_公共科研平台_IT平台 iHuman研究所_PI研究组_徐菲组 iHuman研究所_PI研究组_陶厚朝组 iHuman研究所_PI研究组_赵素文组生命科学与技术学院_硕士生
通讯作者	Zhao, Fei; Tao, Houchao
作者单位	1.ShanghaiTech Univ, iHuman Inst, Ren Bldg,393 Middle Huaxia Rd, Shanghai 201210, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, 555 Zuchongzhi Rd,Bldg 3,Room 426, Shanghai 201203, Peoples R China 3.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China 4.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 201210, Peoples R China
第一作者单位	iHuman研究所; 生命科学与技术学院
通讯作者单位	iHuman研究所
第一作者的第一单位	iHuman研究所
推荐引用方式 GB/T 7714	Xue, Dongxiang,Ye, Lintao,Zheng, Jun,et al. The structure-based traceless specific fluorescence labeling of the smoothened receptor[J]. ORGANIC & BIOMOLECULAR CHEMISTRY,2019,17(25):6136-6142.
APA	Xue, Dongxiang.,Ye, Lintao.,Zheng, Jun.,Wu, Yiran.,Zhang, Xianjun.,...&Tao, Houchao.(2019).The structure-based traceless specific fluorescence labeling of the smoothened receptor.ORGANIC & BIOMOLECULAR CHEMISTRY,17(25),6136-6142.
MLA	Xue, Dongxiang,et al."The structure-based traceless specific fluorescence labeling of the smoothened receptor".ORGANIC & BIOMOLECULAR CHEMISTRY 17.25(2019):6136-6142.