tetano
Editor, Senior Moderator
J Biochem Mol Toxicol
. 2021 Nov 10;e22948.
doi: 10.1002/jbt.22948. Online ahead of print.
Antiviral drugs suppress infection of 2019-nCoV spike pseudotyped virus by interacting with ACE2 protein
Jue Wang[SUP] 1 [/SUP], Yongjing Zhang[SUP] 1 [/SUP], Shiling Hu[SUP] 1 [/SUP], Haoyun Bai[SUP] 1 [/SUP], Zhuoyin Xue[SUP] 1 [/SUP], Yanhong Liu[SUP] 1 [/SUP], Weina Ma[SUP] 1 [/SUP]
Affiliations
Abstract
The outbreak of coronavirus disease 2019 (COVID-19) has induced a large number of deaths worldwide. Angiotensin-converting enzyme 2 (ACE2) is the entry receptor for the 2019 novel coronavirus (2019-nCoV) to infect the host cells. Therefore, ACE2 may be an important target for the prevention and treatment of COVID-19. The aim of this study was to investigate the inhibition effect of valaciclovir hydrochloride (VACV), zidovudine (ZDV), saquinavir (SQV), and efavirenz (EFV) on 2019-nCoV infection. The results of molecule docking and surface plasmon resonance showed that VACV, ZDV, SQV, and EFV could bind to ACE2 protein, with the K[SUB]D[/SUB] value of (4.33 ± 0.09) e[SUP]-8[/SUP] , (6.29 ± 1.12) e[SUP]-6[/SUP] , (2.37 ± 0.59) e[SUP]-5[/SUP] , and (4.85 ± 1.57) e[SUP]-5[/SUP] M, respectively. But only ZDV and EFV prevent the 2019-nCoV spike pseudotyped virus to enter ACE2-HEK293T cells with an EC[SUB]50[/SUB] value of 4.30 ± 1.46 and 3.92 ± 1.36 μM, respectively. ZDV and EFV also have a synergistic effect on preventing entry of virus into cells. In conclusion, ZDV and EFV suppress 2019-nCoV infection of ACE2-HEK293T cells by interacting with ACE2.
Keywords: 2019-nCoV; ACE2; efavirenz; zidovudine.
. 2021 Nov 10;e22948.
doi: 10.1002/jbt.22948. Online ahead of print.
Antiviral drugs suppress infection of 2019-nCoV spike pseudotyped virus by interacting with ACE2 protein
Jue Wang[SUP] 1 [/SUP], Yongjing Zhang[SUP] 1 [/SUP], Shiling Hu[SUP] 1 [/SUP], Haoyun Bai[SUP] 1 [/SUP], Zhuoyin Xue[SUP] 1 [/SUP], Yanhong Liu[SUP] 1 [/SUP], Weina Ma[SUP] 1 [/SUP]
Affiliations
- PMID: 34755435
- DOI: 10.1002/jbt.22948
Abstract
The outbreak of coronavirus disease 2019 (COVID-19) has induced a large number of deaths worldwide. Angiotensin-converting enzyme 2 (ACE2) is the entry receptor for the 2019 novel coronavirus (2019-nCoV) to infect the host cells. Therefore, ACE2 may be an important target for the prevention and treatment of COVID-19. The aim of this study was to investigate the inhibition effect of valaciclovir hydrochloride (VACV), zidovudine (ZDV), saquinavir (SQV), and efavirenz (EFV) on 2019-nCoV infection. The results of molecule docking and surface plasmon resonance showed that VACV, ZDV, SQV, and EFV could bind to ACE2 protein, with the K[SUB]D[/SUB] value of (4.33 ± 0.09) e[SUP]-8[/SUP] , (6.29 ± 1.12) e[SUP]-6[/SUP] , (2.37 ± 0.59) e[SUP]-5[/SUP] , and (4.85 ± 1.57) e[SUP]-5[/SUP] M, respectively. But only ZDV and EFV prevent the 2019-nCoV spike pseudotyped virus to enter ACE2-HEK293T cells with an EC[SUB]50[/SUB] value of 4.30 ± 1.46 and 3.92 ± 1.36 μM, respectively. ZDV and EFV also have a synergistic effect on preventing entry of virus into cells. In conclusion, ZDV and EFV suppress 2019-nCoV infection of ACE2-HEK293T cells by interacting with ACE2.
Keywords: 2019-nCoV; ACE2; efavirenz; zidovudine.