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International Journal of Molecular Sciences

International Journal of Molecular Sciences

IF: 4.9
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25-Hydroxycholesterol-Conjugated EK1 Peptide with Potent and Broad-Spectrum Inhibitory Activity against SARS-CoV-2, Its Variants of Concern, and Other Human Coronaviruses

Published:1 November 2021 DOI: 10.3390/ijms222111869 PMID: 34769299
Qiaoshuai Lan, Chao Wang, Jie Zhou, Lijue Wang, Fanke Jiao, Yanbo Zhang, Yanxing Cai, Lu Lu, Shuai Xia, Shibo Jiang

Abstract

The COVID-19 pandemic caused by SARS-CoV-2 infection poses a serious threat to global public health and the economy. The enzymatic product of cholesterol 25-hydroxylase (CH25H), 25-Hydroxycholesterol (25-HC), was reported to have potent anti-SARS-CoV-2 activity. Here, we found that the combination of 25-HC with EK1 peptide, a pan-coronavirus (CoV) fusion inhibitor, showed a synergistic antiviral activity. We then used the method of 25-HC modification to design and synthesize a series of 25-HC-modified peptides and found that a 25-HC-modified EK1 peptide (EK1P4HC) was highly effective against infections caused by SARS-CoV-2, its variants of concern (VOCs), and other human CoVs, such as HCoV-OC43 and HCoV-229E. EK1P4HC could protect newborn mice from lethal HCoV-OC43 infection, suggesting that conjugation of 25-HC with a peptide-based viral inhibitor was a feasible and universal strategy to improve its antiviral activity.

Substances (4)

Materials
Procduct Name CAS Molecular Formula Supplier Price
25-HYDROXYCHOLESTEROL 2140-46-7 C27H46O2 246 suppliers $15.00-$1880.00
25-HYDROXYCHOLESTEROL 2140-46-7 C27H46O2 246 suppliers $15.00-$1880.00
25-HYDROXYCHOLESTEROL 2140-46-7 C27H46O2 246 suppliers $15.00-$1880.00
25-HYDROXYCHOLESTEROL 2140-46-7 C27H46O2 246 suppliers $15.00-$1880.00

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