Damien Bonnard, Erwann Le Rouzic, Matthew R Singer, Zhe Yu, Frédéric Le Strat, Claire Batisse, Julien Batisse, Céline Amadori, Sophie Chasset, Valerie E Pye, Stéphane Emiliani, Benoit Ledoussal, Marc Ruff, François Moreau, Peter Cherepanov, Richard Benarous
HIV-1 integrase-LEDGF allosteric inhibitors (INLAIs) share the binding site on the viral protein with the host factor LEDGF/p75. These small molecules act as molecular glues promoting hyper-multimerization of HIV-1 IN protein to severely perturb maturation of viral particles. Herein, we describe a new series of INLAIs based on a benzene scaffold that display antiviral activity in the single digit nanomolar range. Akin to other compounds of this class, the INLAIs predominantly inhibit the late stages of HIV-1 replication...
June 13, 2023: Antimicrobial Agents and Chemotherapy