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Two anti-inflammatory drug - Carprofen and Celecoxib - may inhibit a key enzyme in the replication and transcription of the virus responsible for COVID-19, according to the study, published in the International Journal of Molecular Sciences.
Key Findings:
• The researchers from Universitat Rovira in Spain used computer techniques to analyze 6,466 drugs authorized by various drug agencies for both human and veterinary use.
• Assessed whether these drugs could be used to inhibit the main protease of the virus (M-pro) enzyme, which plays an essential role in the replication of the virus.
• Some of the trials coordinated by the WHO against the COVID-19 pandemic also aim to inhibit M-pro using two antiretrovirals such as Lopinavir and Ritonavir (drugs initially designed to treat HIV).
• As a result of the study, the researchers predicted that 7 of these 6,466 drugs may inhibit M-pro.
• The results have been shared with the international initiative COVID Moonshot which has selected 2 of these 7 compounds (i.e., Carprofen and Celecoxib) in order to test their ability to inhibit M-pro in vitro.
• The results obtained show that at a concentration of 50 uM of Celecoxib or Carprofen, the inhibition of the in vitro activity of M-pro is 11.90 and 4.0%, respectively.
• Therefore, both molecules could be used as a starting point for further lead optimization to obtain even more potent derivatives.
Source: https://www.eurekalert.org/pub_releases/2020-05/uriv-tad052720.php
Key Findings:
• The researchers from Universitat Rovira in Spain used computer techniques to analyze 6,466 drugs authorized by various drug agencies for both human and veterinary use.
• Assessed whether these drugs could be used to inhibit the main protease of the virus (M-pro) enzyme, which plays an essential role in the replication of the virus.
• Some of the trials coordinated by the WHO against the COVID-19 pandemic also aim to inhibit M-pro using two antiretrovirals such as Lopinavir and Ritonavir (drugs initially designed to treat HIV).
• As a result of the study, the researchers predicted that 7 of these 6,466 drugs may inhibit M-pro.
• The results have been shared with the international initiative COVID Moonshot which has selected 2 of these 7 compounds (i.e., Carprofen and Celecoxib) in order to test their ability to inhibit M-pro in vitro.
• The results obtained show that at a concentration of 50 uM of Celecoxib or Carprofen, the inhibition of the in vitro activity of M-pro is 11.90 and 4.0%, respectively.
• Therefore, both molecules could be used as a starting point for further lead optimization to obtain even more potent derivatives.
Source: https://www.eurekalert.org/pub_releases/2020-05/uriv-tad052720.php
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