FIG 5.
Comparison of the antiviral activities of LEN and KFA-012 against WT and CA mutants. (A) Chemical structure of LEN. (B) Chemical structure of the modified LEN-like compound KFA-012. (C) Early stage antiviral activities of LEN and KFA-012 were measured against pseudotyped HIV-1NL4-3_RFP in MT-4 cells. P values in blue and green indicate differences compared to WT for LEN and KFA-012, respectively; P values in red show the statistical significance for the fold increases of the KFA-012 potency versus LEN potency with respect to the indicated CA variants. (D) X-ray crystal structure of the cross-linked CA(WT) hexamer (light green/peach) in complex with KFA-012 (dark purple) with the 2Fo-Fc density scaled to 1σ (blue mesh; PDB: 7RMJ). (E) Superimposition of cross-linked CA(WT) hexamer in complex with KFA-012 (PDB: 7RMJ; light green + dark purple) and LEN (PDB 6VKV; gray + orange).