Synthesis of maleimide-braced peptide macrocycles and their potential anti-SARS-CoV-2 mechanisms
文献类型：期刊论文
| 作者 | Li, Jian1,2; Sun, Jina2,3; Zhang, Xianglei4,5; Zhang, Ruxue6; Wang, Qian1,2; Wang, Lin4,5; Zhang, Leike6; Xie, Xiong2,3; Li, Chunpu2,3; Zhou, Yu2,3
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| 刊名 | CHEMICAL COMMUNICATIONS
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| 出版日期 | 2022-12-12 |
| 页码 | 4 |
| ISSN号 | 1359-7345 |
| DOI | 10.1039/d2cc06371a |
| 通讯作者 | Xiao, Gengfu(xiaogf@wh.iov.cn) ; Bai, Fang(baifang@shanghaitech.edu.cn) ; Liu, Hong(hliu@simm.ac.cn) |
| 英文摘要 | Macrocycles often exhibit good biological properties and potential druggability, which lead to versatile applications in the pharmaceutical industry. Herein, we report a highly efficient and practical methodology for the functionalization and macrocyclization of Trp and Trp-containing peptides via Pd(ii)-catalyzed C-H alkenylation at the Trp C4 position. This method provides direct access to C4 maleimide-decorated Trp-containing peptidomimetics and maleimide-braced 17- to 30-membered peptide macrocycles. In particular, these unique macrocycles revealed low micro- to sub-micromolar EC50 values with promising anti-SARS-CoV-2 activities. Further explorations with computational methodologies and experimental validations indicated that these macrocycles exert antiviral effects through binding with the N protein of SARS-CoV-2. |
| WOS关键词 | C-H ACTIVATION ; FUNCTIONALIZATION ; TRYPTOPHAN |
| 资助项目 | National Natural Science Foundation of China[82130105] ; National Natural Science Foundation of China[82173654] ; National Natural Science Foundation of China[82003654] ; National Natural Science Foundation of China[31970165] ; Strategic Priority Research Program of Chinese Academy of Sciences[SIMM020102] ; Science and Technology Commission of Shanghai Municipality grants[20430780300] ; Shanghai Science and Technology Development Funds[20QA1406400] ; China Postdoctoral Science Foundation[2021M693170] ; National Key Research and Development Program of China[2021YFC2300700] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| 出版者 | ROYAL SOC CHEMISTRY |
| WOS记录号 | WOS:000901671800001 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/304201]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Xiao, Gengfu; Bai, Fang; Liu, Hong |
| 作者单位 | 1.Nanjing Univ Chinese Med, Sch Chinese Mat Med, 138 Xianlin Ave, Nanjing 210023, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China 3.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China 4.ShanghaiTech Univ, Shanghai Inst Adv Immunochem Studies, Shanghai 201210, Peoples R China 5.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 201210, Peoples R China 6.Chinese Acad Sci, Wuhan Inst Virol, Ctr Biosafety Mega Sci, State Key Lab Virol, Wuhan 430071, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Jian,Sun, Jina,Zhang, Xianglei,et al. Synthesis of maleimide-braced peptide macrocycles and their potential anti-SARS-CoV-2 mechanisms[J]. CHEMICAL COMMUNICATIONS,2022:4. |
| APA | Li, Jian.,Sun, Jina.,Zhang, Xianglei.,Zhang, Ruxue.,Wang, Qian.,...&Liu, Hong.(2022).Synthesis of maleimide-braced peptide macrocycles and their potential anti-SARS-CoV-2 mechanisms.CHEMICAL COMMUNICATIONS,4. |
| MLA | Li, Jian,et al."Synthesis of maleimide-braced peptide macrocycles and their potential anti-SARS-CoV-2 mechanisms".CHEMICAL COMMUNICATIONS (2022):4. |
入库方式： OAI收割
来源：上海药物研究所
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