期刊
ADVANCED THERAPEUTICS
卷 4, 期 5, 页码 -出版社
WILEY
DOI: 10.1002/adtp.202000224
关键词
estradiol benzoate; fusion inhibitor; itraconazole; SARS-CoV-2; spike
资金
- National Natural Science Foundation of China [32041005]
- Major scientific and technological projects of Guangdong Province [2019B020202002]
- China Academy of Traditional Chinese Medicine [ZZ13-035-02, 2019XZZX-LG04]
- Fund of Natural Science Foundation of Guangdong Province [2018A030313056, 202020012611500005]
- Guangzhou Science and Technology Program [201904010477, 2020B111110001]
The study found that Itraconazole and Estradiol benzoate can inhibit viral entry by targeting the six-helix fusion core of SARS-CoV-2 S protein, presenting them as novel potential therapeutic remedies for COVID-19 treatment. Further research also showed that Itraconazole has broad-spectrum activity targeting 6-HB in the S2 subunit of SARS-CoV and MERS-CoV S protein, suggesting its potential as a pan-coronavirus fusion inhibitor.
SARS-CoV-2 caused the emerging epidemic of coronavirus disease in 2019 (COVID-19). To date, there are more than 82.9 million confirmed cases worldwide, there is no clinically effective drug against SARS-CoV-2 infection. The conserved properties of the membrane fusion domain of the spike (S) protein across SARS-CoV-2 make it a promising target to develop pan-CoV therapeutics. Herein, two clinically approved drugs, Itraconazole (ITZ) and Estradiol benzoate (EB), are found to inhibit viral entry by targeting the six-helix (6-HB) fusion core of SARS-CoV-2 S protein. Further studies shed light on the mechanism that ITZ and EB can interact with the heptad repeat 1 (HR1) region of the spike protein, to present anti-SARS-CoV-2 infections in vitro, indicating they are novel potential therapeutic remedies for COVID-19 treatment. Furthermore, ITZ shows broad-spectrum activity targeting 6-HB in the S2 subunit of SARS-CoV and MERS-CoV S protein, inspiring that ITZ have the potential for development as a pan-coronavirus fusion inhibitor.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据