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The COVID-19 pandemic has raged across the globe for more than two years, infecting hundreds of millions and killing millions
However, it should be noted that most of the existing new crown vaccines are developed based on the original virus strain of the new crown, and the effectiveness of these new crown variants is constantly decreasing
Most of the existing new crown vaccines are developed based on the original new crown virus strains, and the effectiveness of these new crown variants is constantly decreasing
In response to emerging Covid-19 variants, developing a broad-spectrum Covid-19 treatment will be key to containing the COVID-19 pandemic
Recently, researchers from Columbia University and Cornell University published in Nature titled: A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic (TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic and therapeutic drugs)
A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic
The research developed a small molecule compound that inhibits TMPRSS2, N-0385, which can prevent the infection and invasion process of the new coronavirus and its variant strains (including Delta and Omicron)
The life cycle of SARS-CoV-2 begins with attachment and entry into respiratory epithelial cells via angiotensin-converting enzyme 2 (ACE2) receptors
To put it vividly, if ACE2 is compared to "door handle", then TMPRSS2 is "lubricating oil"
In this latest study, the research team developed a small library of peptidomimetic compounds to screen for inhibitors of TMPRSS2 proteolytic activity
Research team screened peptidomimetic drugs that inhibit TMPRSS2
Research team screened peptidomimetic drugs that inhibit TMPRSS2In in vitro cell experiments, N-0385 inhibited SARS-CoV-2 infection by 99%, and its half effective concentration (EC50) was 2.
More importantly, N-0385 has strong anti-infective efficacy against several common SARS-CoV-2 variants such as Delta and Omicron
Anti-TMPRSS2 peptidomimetics such as N-0385 are low nanomolar inhibitors of SARS-CoV-2
Anti-TMPRSS2 peptidomimetics such as N-0385 are low nanomolar inhibitors of SARS-CoV-2Subsequently, the research team further tested the therapeutic effect of N-0385 in an ACE2 transgenic mouse model capable of infecting SARS-CoV-2
N-0385 reduces infection and improves survival in mice
N-0385 reduces infection and improves survival in miceNot only that, the surviving mice treated with N-0385 were in better physiological state, with tissue morphology tending to be pre-infection
N-0385 has inhibitory effect on four new coronavirus variants
N-0385 has inhibitory effect on four new coronavirus variantsOverall, this study reports an inhibitor targeting TMPRSS2, N-0385, a peptidomimetic drug that blocks key steps in viral invasion, effectively inhibits 2019-nCoV infection, and reduces SARS-CoV-2 infection in mouse experiments.
More importantly, N-0385 has good anti-infective efficacy against various new coronavirus variants (such as Delta and Omicron), providing a new and effective prevention and early treatment for the infection of the new coronavirus and its variants select
N-0385 has good anti-infective efficacy against various new coronavirus variants (such as Delta and Omicron), providing a new and effective prevention and early treatment option for the infection of the new coronavirus and its variants
Original source:
Original Source: Original Source:Shapira, T.
Shapira, T.
, Monreal, IA, Dion, SP et al.
A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic .
Nature (2022).
https://doi.
org/10.
1038/s41586-022 -04661-w A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic
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