Tafenoquine and its derivatives as inhibitors for the severe acute respiratory syndrome coronavirus 2.

ABSTRACT: The pandemic caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has severely affected human lives around the world as well as the global economy. Therefore, effective treatments against COVID-19 are urgently needed. Here, we screened a library containing Food and Drug Administration (FDA)-approved compounds to identify drugs that could target the SARS-CoV-2 main protease (M^pro), which is indispensable for viral protein maturation and regard as an important therapeutic target. We identified antimalarial drug tafenoquine (TFQ), which is approved for radical cure of Plasmodium vivax and malaria prophylaxis, as a top candidate to inhibit M^pro protease activity. The crystal structure of SARS-CoV-2 M^pro in complex with TFQ revealed that TFQ no

SUBMITTER: Chen Y 

PROVIDER: S-EPMC8800562 | biostudies-literature | 2022 Mar

REPOSITORIES: biostudies-literature