Title | Bifunctional Compounds as Molecular Degraders for Integrin-Facilitated Targeted Protein Degradation |
Author | |
Corresponding Author | Hongchang 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
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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 Type | Journal Article |
Identifier | http://kc.sustech.edu.cn/handle/2SGJ60CL/415782 |
Department | Department 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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File Name/Size | DocType | Version | Access | License | ||
Bifunctional Compoun(5591KB) | Open Access | -- | View |
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