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December 18, 2020 // --- COVID-19 caused by sars-CoV-2 virus poses a serious threat to human health and endangers the global economy.
, however, there is currently no effective drug available to treat COVID-19, so there is a great demand for resistance.
By combining computational screening with an effective cell prosthetic virus system, a team led by Professor Yuan Shuguang of the Shenzhen Institute of Advanced Technology (SIAT) of the Chinese Academy of Sciences has confirmed that clinical histone deacetylase (HDAC) inhibitors can be effective in preventing SARS-CoV-2 and may be used against COVID-19.
(Photo Source: Www.pixabay.com) researchers found that several HDAC inhibitors can bind to human angiosin-converting enzyme 2 (ACE2) on the cell surface, leading to changes in the overall structure of ACE2.
because SARS-CoV-2 identifies human ACE2 binders through its hedgehog protein during viral infection, this alternating inhibits the binding of the ACE2-S protein and blocks the entry of SARS-CoV-2 host cells.
the results, the team then screened 18 commercially available HDAC inhibitors and studied their effectiveness in inhibiting SARS-CoV-2 from entering cells.
found that four inhibitors, panobinostat, givinostat, CAY10603 and sirtinol, were significantly effective.
ec50 obtained from these four HDAC drugs is about 3 m, well below EC50 from other drugs (both are greater than 100 sM).
cell signal network analysis revealed the possible mechanisms by which these HDAC inhibitors are effective against SARS-CoV-2.
this work was published as the cover story of ACS Pharmacology and Translational Science.
(Bioon.com) Source: Clinical histone deacetylase inhibitors are effective against COST COVID-19 Source: Ke Liu et al. Clinical HDAC Inhibitors Are Effective Drugs to Prevent the Entry of SARS-CoV2, ACS Pharmacology & Translational Science (2020). DOI: 10.1021/acsptsci.0c00163。