A Palmitic Acid-Conjugated, Peptide-Based pan-CoV Fusion Inhibitor Potently Inhibits Infection of SARS-CoV-2 Omicron and Other Variants of Concern

被引：17

作者：

Lan, Qiaoshuai ^{[1
]}

Chan, Jasper Fuk-Woo ^{[2
,3
,4
]}

Xu, Wei ^{[1
]}

Wang, Lijue ^{[1
]}

Jiao, Fanke ^{[1
]}

Zhang, Guangxu ^{[1
]}

Pu, Jing ^{[1
]}

Zhou, Jie ^{[1
]}

Xia, Shuai ^{[1
]}

Lu, Lu ^{[1
]}

Yuen, Kwok-Yung ^{[2
,3
,4
]}

Jiang, Shibo ^{[1
]}

Wang, Qian ^{[1
]}

机构：

[1] Fudan Univ, Shanghai Frontiers Sci Ctr Pathogen Microbes & In, Sch Basic Med Sci, Shanghai Inst Infect Dis & Biosecur,Key Lab Med M, Shanghai 200032, Peoples R China

[2] Univ Hong Kong, Li Ka Shing Fac Med, Carol Yu Ctr Infect,Pokfulam, Dept Microbiol,State Key Lab Emerging Infect Dis, Hong Kong, Peoples R China

[3] Univ Hong Kong, Dept Clin Microbiol & Infect Control, Shenzhen Hosp, Shenzhen 518000, Peoples R China

[4] Hong Kong Sci & Technol Pk, Ctr Virol Vaccinol & Therapeut, Hong Kong, Peoples R China

来源：

VIRUSES-BASEL | 2022年 / 14卷 / 03期

基金：

中国国家自然科学基金;

关键词：

palmitic acid; lipopeptide; Omicron; beta-coronavirus; entry inhibitor; SPIKE PROTEIN; CORONAVIRUS; SARS; ANTIBODIES; VACCINE;

D O I：

10.3390/v14030549

中图分类号：

Q93 [微生物学];

学科分类号：

071005 ; 100705 ;

摘要：

Our previous studies have shown that cholesterol-conjugated, peptide-based pan-coronavirus (CoV) fusion inhibitors can potently inhibit human CoV infection. However, only palmitic acid (C16)-based lipopeptide drugs have been tested clinically, suggesting that the development of C16based lipopeptide drugs is feasible. Here, we designed and synthesized a C16-modified pan-CoV fusion inhibitor, EK1-C16, and found that it potently inhibited infection by SARS-CoV-2 and its variants of concern (VOCs), including Omicron, and other human CoVs and bat SARS-related CoVs (SARSr-CoVs). These results suggest that EK1-C16 could be further developed for clinical use to prevent and treat infection by the currently circulating MERS-CoV, SARS-CoV-2 and its VOCs, as well as any future emerging or re-emerging coronaviruses.

引用

页数：11

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