A DNA-encoded library for the identification of natural product binders that modulate poly (ADP-ribose) polymerase 1, a validated anti-cancer target

doi:10.1016/j.bbrc.2020.04.022

	A DNA-encoded library for the identification of natural product binders that modulate poly (ADP-ribose) polymerase 1, a validated anti-cancer target
	Li, Jie1,2,3,4 ; Li, Yu1,2,3,4 ; Lu, Fengping1 ; Liu, Lili1 ; Ji, Qun1 ; Song, Ke1 ; Yin, Qianqian1 ; Lerner, Richard A.5; Yang, Guang1 ; Xu, Hongtao1 ; Ma, Peixiang1
	2020-12-03
发表期刊	BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (IF:2.5[JCR-2023],2.7[5-Year])
ISSN	0006-291X
卷号	533 期号:2 页码:241-248
发表状态	已发表
DOI	10.1016/j.bbrc.2020.04.022
摘要	Natural products have been an invaluable source of drug discovery, but their targets remain largely unknown. Natural products enriched DNA-encoded chemical libraries (nDELs) empower the researchers to rapidly and economically screen numerous natural products against various protein targets, and therefore promote the elucidation of the molecular mechanisms. In this work, we used poly (ADP-ribose) polymerase 1 (PARP1), as an example to explore the usage of nDEL for the functional natural products selection. We used late-stage modification approach to label three positive binders with unique DNA barcodes, whose dissociation constants range from sub-micromolar to micromolar. The selection criterion was set up according to the enrichment of these controls. Five natural products selected by this criterion directly bind to PARP1 in SPR, among which luteolin exhibits the highest inhibitory activity against PARP1. Moreover, luteolin selectively induces accumulation of DNA double-strand breaks and G2/M phase arrest in BRCA-deficient cells. All the findings from these investigations on luteolin support that PARP1 inhibition is one of the mechanisms for its anti-cancer activity. (C) 2020 Published by Elsevier Inc.
关键词	DNA-Encoded library Natural products Drug discovery Luteolin PARP1
收录类别	SCI ; SCIE
语种	英语
资助项目	National Natural Science Foundation of China[21977070][U19A2011][31500632] ; Science and Technology Commission of Shanghai Municipality[16DZ1910200]
WOS研究方向	Biochemistry & Molecular Biology ; Biophysics
WOS类目	Biochemistry & Molecular Biology ; Biophysics
WOS记录号	WOS:000583921700008
出版者	ACADEMIC PRESS INC ELSEVIER SCIENCE
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/123933
专题	生命科学与技术学院_硕士生免疫化学研究所_特聘教授组_抗体化学实验室免疫化学研究所_特聘教授组_功能筛选实验室免疫化学研究所_特聘教授组_抗体设计学实验室生命科学与技术学院_博士生免疫化学研究所_公共科研平台_生物医学大数据平台
通讯作者	Xu, Hongtao; Ma, Peixiang
作者单位	1.ShanghaiTech Univ, Shanghai Inst Adv Immunochem Studies, Shanghai 201210, Peoples R China 2.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 201210, Peoples R China 3.Chinese Acad Sci, Inst Biochem & Cell Biol, Shanghai Inst Biol Sci, Shanghai 200031, Peoples R China 4.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 5.Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
第一作者单位	免疫化学研究所; 生命科学与技术学院
通讯作者单位	免疫化学研究所
第一作者的第一单位	免疫化学研究所
推荐引用方式 GB/T 7714	Li, Jie,Li, Yu,Lu, Fengping,et al. A DNA-encoded library for the identification of natural product binders that modulate poly (ADP-ribose) polymerase 1, a validated anti-cancer target[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,2020,533(2):241-248.
APA	Li, Jie.,Li, Yu.,Lu, Fengping.,Liu, Lili.,Ji, Qun.,...&Ma, Peixiang.(2020).A DNA-encoded library for the identification of natural product binders that modulate poly (ADP-ribose) polymerase 1, a validated anti-cancer target.BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,533(2),241-248.
MLA	Li, Jie,et al."A DNA-encoded library for the identification of natural product binders that modulate poly (ADP-ribose) polymerase 1, a validated anti-cancer target".BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS 533.2(2020):241-248.