Structural and Druggability Landscape of Frizzled G Protein-Coupled Receptors

doi:10.1016/j.tibs.2018.09.002

	Structural and Druggability Landscape of Frizzled G Protein-Coupled Receptors
	Zhang, Xianjun1,2,3 ; Dong, Shaowei1,2,3 ; Xu, Fei1
	2018-12
发表期刊	TRENDS IN BIOCHEMICAL SCIENCES (IF:11.6[JCR-2023],12.5[5-Year])
ISSN	0968-0004
卷号	43 期号:12 页码:1033-1046
发表状态	已发表
DOI	10.1016/j.tibs.2018.09.002
摘要	Class Frizzled G protein-coupled receptors (GPCRs), which includes the Smoothened receptor (SMO) and 10 Frizzled receptors (FZDs), are responsible for mediating fundamental signaling in embryonic development and tissue homeostasis. Dysregulation of these receptors can lead to cancer. Structural understanding of these molecules has provided insight to their function and signaling, and guided drug discovery. To date, the structures of the multi-and individual domains of SMO, 14 FZD extracellular domains, and the transmembrane domain (TMD) of FZD4, have been reported. Here, we review all reported frizzled family structures and diverse signalosome models, with an emphasis on the different ligand binding sites and lipid binding grooves, aiming to uncover the druggability landscape of the frizzled GPCR family.
收录类别	SCI ; SCIE
语种	英语
WOS研究方向	Biochemistry & Molecular Biology
WOS类目	Biochemistry & Molecular Biology
WOS记录号	WOS:000450911400009
出版者	ELSEVIER SCIENCE LONDON
WOS关键词	WNT PATHWAY ; RECOGNITION ; INHIBITOR ; BINDING ; SIGNALOSOME ; RESISTANCE ; CANCER ; NORRIN
原始文献类型	Review
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/28688
专题	生命科学与技术学院_博士生 iHuman研究所_PI研究组_徐菲组
通讯作者	Xu, Fei
作者单位	1.ShanghaiTech Univ, Sch Life Sci & Technol, iHuman Inst, Shanghai 201210, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Biochem & Cell Biol, Shanghai 200031, Peoples R China 3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
第一作者单位	生命科学与技术学院
通讯作者单位	生命科学与技术学院
第一作者的第一单位	生命科学与技术学院
推荐引用方式 GB/T 7714	Zhang, Xianjun,Dong, Shaowei,Xu, Fei. Structural and Druggability Landscape of Frizzled G Protein-Coupled Receptors[J]. TRENDS IN BIOCHEMICAL SCIENCES,2018,43(12):1033-1046.
APA	Zhang, Xianjun,Dong, Shaowei,&Xu, Fei.(2018).Structural and Druggability Landscape of Frizzled G Protein-Coupled Receptors.TRENDS IN BIOCHEMICAL SCIENCES,43(12),1033-1046.
MLA	Zhang, Xianjun,et al."Structural and Druggability Landscape of Frizzled G Protein-Coupled Receptors".TRENDS IN BIOCHEMICAL SCIENCES 43.12(2018):1033-1046.