中文版 | English
Title

Bifunctional Compounds as Molecular Degraders for Integrin-Facilitated Targeted Protein Degradation

Author
Corresponding AuthorHongchang Li; Liang Chen; Lijing Fang
Publication Years
2022-11-23
DOI
Source Title
ISSN
0002-7863
EISSN
1520-5126
Abstract
As effective ways to regulate protein levels, targeted protein degradation technologies have attracted great attention in recent years. Here, we established a novel integrin-facilitated lysosomal degradation (IFLD) strategy to degrade extracellular and cell membrane proteins using bifunctional compounds as molecular degraders. By conjugation of a target protein-binding ligand with an integrin-recognition ligand, the resulting molecular degrader proved to be highly efficient to induce the internalization and subsequent degradation of extracellular or cell membrane proteins in an integrin-and lysosome-dependent manner. As demonstrated in the development of BMS-L1-RGD, which is an efficient programmed death-ligand 1 (PD-L1) degrader validated both in vitro and in vivo, the IFLD strategy expands the toolbox for regulation of secreted and membrane-associated proteins and thus has great potential to be applied in chemical biology and drug discovery.
URL[Source Record]
Indexed By
Language
English
Important Publications
NI Journal Papers
SUSTech Authorship
Others
Funding Project
[2021YFA0910000] ; [2020YFA0710802] ; [21977111] ; [22007096] ; [2019A1515012073] ; [2022A1515012030] ; [GJHZ20210705141407022] ; [JCYJ20210324120200001] ; [JCYJ20210324105007019]
WOS Research Area
Chemistry
WOS Subject
Chemistry, Multidisciplinary
WOS Accession No
WOS:000889821600001
Publisher
Data Source
人工提交
Publication Status
在线出版
Citation statistics
Cited Times [WOS]:1
Document TypeJournal Article
Identifierhttp://kc.sustech.edu.cn/handle/2SGJ60CL/415782
DepartmentDepartment of Biochemistry
南方科技大学医学院
Affiliation
1.Institute of Biomedicine and Biotechnology, Shenzhen Institute of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, Guangdong, China
2.Department of Biochemistry, School of Medicine, Southern University of Science and Technology, Shenzhen, 518055, Guangdong, China
Recommended Citation
GB/T 7714
Jiwei Zheng,Wanyi He,Jing Li,et al. Bifunctional Compounds as Molecular Degraders for Integrin-Facilitated Targeted Protein Degradation[J]. Journal of the American Chemical Society,2022.
APA
Jiwei Zheng.,Wanyi He.,Jing Li.,Xuejia Feng.,Yanyan Li.,...&Lijing Fang.(2022).Bifunctional Compounds as Molecular Degraders for Integrin-Facilitated Targeted Protein Degradation.Journal of the American Chemical Society.
MLA
Jiwei Zheng,et al."Bifunctional Compounds as Molecular Degraders for Integrin-Facilitated Targeted Protein Degradation".Journal of the American Chemical Society (2022).
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