A new class of capsid-targeting inhibitors that specifically block HIV-1 nuclear import

Abstract excerpt

Abstract HIV-1 capsids cross nuclear pore complexes (NPCs) by engaging with the nuclear import machinery. To identify compounds that inhibit HIV-1 nuclear import, we screened drugs in silico on a three-dimensional model of a CA hexamer bound by Transportin-1 (TRN-1). Among hits, compound H27 inhibited HIV-1 with a low micromolar IC 50 . Unlike other CA-targeting compounds, H27 did not alter CA assembly or...