Constructing Head-to-Tail Cyclic Peptide DNA-Encoded Libraries Using Two-Directional Synthesis Strategy
文献类型：期刊论文
| 作者 | Liu, Wang1,3,4; Bai, Xiaopeng2; Song, Liping3; Wang, Xuan1; Lu, Xiaojie1,4
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| 刊名 | BIOCONJUGATE CHEMISTRY
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| 出版日期 | 2022-04-20 |
| 卷号 | 33期号:4页码:560-565 |
| ISSN号 | 1043-1802 |
| DOI | 10.1021/acs.bioconjchem.2c00078 |
| 通讯作者 | Song, Liping(lpsong@shu.edu.cn) ; Wang, Xuan(wangxuan2@simm.ac.cn) ; Lu, Xiaojie(xjlu@simm.ac.cn) |
| 英文摘要 | Macrocyclic peptides are an important class of therapeutic agents for the biological targets that are difficult to modulate by small-molecule compounds. Meanwhile, DNA-encoded library technology (DELT) provides a powerful platform for hits discovery. The unity of both fields has proven highly productive in finding cyclic peptide hits against diverse pharmaceutical proteins. Many researchers have extended the chemical toolbox for constructing head-to-tail macrocyclic DNA-encoded libraries with various ring sizes. However, the linear peptides of different lengths necessitate tuning the distance between closing sites and DNA-linked sites to perform the macrocyclization process, presumably due to the constrained conformation of linear precursors. To tackle this issue and streamline the synthetic workflow, we report a two-directional synthesis strategy. This method starts from a trifunctional reagent and prepares DNA-linked macrocyclic peptides of ring size between 15 (5-leer) and 24 (8-leer) via amide bond formation reaction, a common method to create macrocyclic peptides. |
| WOS关键词 | INHIBITORS |
| 资助项目 | National Science & Technology Major Project Key New Drug Creation and Manufacturing Program, China[2018ZX09711002-005] ; Shanghai Commission of Science and Technology[18431907100] ; [NSFC-21877117] ; [91953203] ; [NSFC-21907103] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000791363400004 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/299385]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Song, Liping; Wang, Xuan; Lu, Xiaojie |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 2.UCB, 87 Cambridge Pk Dr, Cambridge, MA 02140 USA 3.Shanghai Univ, Coll Sci, Dept Chem, Shanghai 200444, Peoples R China 4.Univ Chinese Acad Sci, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu, Wang,Bai, Xiaopeng,Song, Liping,et al. Constructing Head-to-Tail Cyclic Peptide DNA-Encoded Libraries Using Two-Directional Synthesis Strategy[J]. BIOCONJUGATE CHEMISTRY,2022,33(4):560-565. |
| APA | Liu, Wang,Bai, Xiaopeng,Song, Liping,Wang, Xuan,&Lu, Xiaojie.(2022).Constructing Head-to-Tail Cyclic Peptide DNA-Encoded Libraries Using Two-Directional Synthesis Strategy.BIOCONJUGATE CHEMISTRY,33(4),560-565. |
| MLA | Liu, Wang,et al."Constructing Head-to-Tail Cyclic Peptide DNA-Encoded Libraries Using Two-Directional Synthesis Strategy".BIOCONJUGATE CHEMISTRY 33.4(2022):560-565. |
入库方式： OAI收割
来源：上海药物研究所
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