Identification of a novel binding inhibitor that blocks the interaction between hSCARB2 and VP1 of enterovirus 71.

ABSTRACT: Enterovirus 71 (EV-A71) infection causes severe hand-foot-and-mouth disease that leads to cardiopulmonary complications and death in young children under 5 years of age. Although there are available vaccines for EV-A71 C⁴, however, there are no efficient drugs for severe cases. Thus, there is an urgent need to find new direct-antiviral agents (DAAs) to control EV-A71 infection. In this study, we report our discovery of the EV-A71 capsid inhibitor PTC-209HBr, a small-molecule Bmi-1 inhibitor and an anticancer agent, and its derivatives that inhibit multiple enteroviruses with an EC₅₀ at a submicromolar efficacy. The mechanism of action of PTC-209HBr was confirmed by time-of-addition, resistance selection and reverse genetics experiments, microscale thermophoresis (MST)

SUBMITTER: Tang Q 

PROVIDER: S-EPMC10120312 | biostudies-literature | 2022 Apr

REPOSITORIES: biostudies-literature