Neutralizing SARS-CoV-2 by dimeric side chain-to-side chain cross-linked ACE2 peptide mimetics

被引:3
|
作者
Zhang, Yan-Ni [1 ,2 ]
Zhang, Yuwei [3 ]
Su, Shan [4 ,5 ]
Zhu, Han-Ying [1 ,2 ]
Xu, Wei [4 ,5 ]
Wang, Lu [3 ]
Wu, Meng [1 ,2 ]
Chen, Kai [1 ,2 ]
Yu, Fei-Qiang [1 ,2 ]
Xi, Tong-Kuai [1 ,2 ]
Zhou, Qin [1 ,2 ]
Xie, You-Hua [4 ,5 ]
Qin, Ximing [1 ,2 ]
Ge, Honghua [1 ,2 ]
Lu, Lu [4 ,5 ]
Qing, Jie [3 ]
Fang, Ge-Min [1 ,2 ]
机构
[1] Anhui Univ, Inst Phys Sci, Dept Hlth Sci, Hefei 230601, Peoples R China
[2] Anhui Univ, Inst Informat, Dept Hlth Sci, Hefei 230601, Peoples R China
[3] Southwest Med Univ, Affiliated Tradit Chinese Med Hosp, Natl Tradit Chinese Med Clin Res Base, Luzhou 646000, Peoples R China
[4] Fudan Univ, Shanghai Inst Infect Dis & Biosecur, Sch Basic Med Sci, Key Lab Med Mol Virol MOE NHC CAMS, Shanghai 200032, Peoples R China
[5] Fudan Univ, Shanghai Inst Infect Dis & Biosecur, Biosafety Level Lab 3, Shanghai 200032, Peoples R China
基金
中国国家自然科学基金;
关键词
CHEMICAL-SYNTHESIS; PROTEINS; INHIBITION; ENTRY; DNA;
D O I
10.1039/d1cc06301d
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
We present the finding of a dimeric ACE2 peptide mimetic designed through side chain cross-linking and covalent dimerization. It has a binding affinity of 16 nM for the SARS-CoV-2 spike RBD, and effectively inhibits the SARS-CoV-2 pseudovirus in Huh7-hACE2 cells with an IC50 of 190 nM and neutralizes the authentic SARS-CoV-2 in Caco2 cells with an IC50 of 2.4 mu M. Our study should provide a new insight for the optimization of peptide-based anti-SARS-CoV-2 inhibitors.
引用
收藏
页码:1804 / 1807
页数:4
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