Article
Structural Impact of Ex Vivo Resistance Mutations on HIV-1 Integrase Polymers Induced by Allosteric Inhibitors.
Journal of molecular biology - 1 Sept 2025
Montermoso Saira, Eilers Grant, Allen Audrey, Sharp Robert, Hwang Young, Bushman Frederic D, Gupta Kushol, Duyne Gregory Van
Abstract excerpt
HIV-1 integrase (IN) is targeted by two classes of antivirals: integrase strand transfer inhibitors (INSTIs), which bind to the active site within the catalytic core domain (CCD), and allosteric integrase inhibitors (ALLINIs), which bind at the CCD dimer interface. ALLINIs were initially designed to disrupt interactions with the cellular cofactor LEDGF/p75, but it has become clear that ALLINIs primarily act by...
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