Quantitative Validation and Application of the Photo-Cross-Linking Selection for Double-Stranded DNA-Encoded Libraries
文献类型：期刊论文
| 作者 | Wu, Xinyuan1,2; Chen, Yujie1,2; Lu, Weiwei2; Jin, Rui2; Lu, Xiaojie1,2
|
| 刊名 | BIOCONJUGATE CHEMISTRY
 |
| 出版日期 | 2022-10-05 |
| 页码 | 7 |
| ISSN号 | 1043-1802 |
| DOI | 10.1021/acs.bioconjchem.2c00421 |
| 通讯作者 | Lu, Xiaojie(xjlu@simm.ac.cn) |
| 英文摘要 | The DNA-encoded compound library (DEL) technology has accelerated the target hits discovery in new drug development. While affinity-based DEL selection can distinguish high-affinity ligands, moderate-affinity ligands are also potential drug candidates with further modifications. Herein, we designed a photo-cross-linking selection method for DELs with double stranded DNA (dsDELs) to screen moderate-affinity ligands. We constructed two photo-cross-linking libraries with linkers of different lengths that connect a diazirine group to the DNA encoded compound. The diazirine group can be activated by UV irradiation and thus bond with the target protein in a reachable distance. In the model selection, the feasibility of the photo-cross linking screening system was verified by qPCR and NGS technology. Both high-affinity and moderate-affinity ligands were successfully selected from the libraries. |
| WOS关键词 | PROTEINS ; STRATEGIES |
| 资助项目 | Shanghai Municipal Science and Technology Major Project ; [NSFC-91953203] ; [NSFC-21877117] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000866364700001 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/302769]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Lu, Xiaojie |
| 作者单位 | 1.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wu, Xinyuan,Chen, Yujie,Lu, Weiwei,et al. Quantitative Validation and Application of the Photo-Cross-Linking Selection for Double-Stranded DNA-Encoded Libraries[J]. BIOCONJUGATE CHEMISTRY,2022:7. |
| APA | Wu, Xinyuan,Chen, Yujie,Lu, Weiwei,Jin, Rui,&Lu, Xiaojie.(2022).Quantitative Validation and Application of the Photo-Cross-Linking Selection for Double-Stranded DNA-Encoded Libraries.BIOCONJUGATE CHEMISTRY,7. |
| MLA | Wu, Xinyuan,et al."Quantitative Validation and Application of the Photo-Cross-Linking Selection for Double-Stranded DNA-Encoded Libraries".BIOCONJUGATE CHEMISTRY (2022):7. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。