Antiviral Activity and Crystal Structures of HIV-1 gp120 Antagonists.

ABSTRACT: As part of our effort to discover drugs that target HIV-1 entry, we report the antiviral activity and crystal structures of two novel inhibitors in a complex with a gp120 core. NBD-14204 showed similar antiviral activity against all the clinical isolates tested. The IC₅₀ values were in the range of 0.24-0.9 µM with an overall mean of 0.47 ± 0.03 µM, showing slightly better activity against the clinical isolates than against the lab-adapted HIV-1_HXB2 (IC₅₀ = 0.96 ± 0.1 µM)_. Moreover, the antiviral activity of NBD-14208 was less consistent, showing a wider range of IC₅₀ values (0.66-5.7 µM) with an overall mean of 3 ± 0.25 µM and better activity against subtypes B and D (Mean IC₅₀ 2.2-2.5 µM) than the A, C and Rec viruses (Mea

SUBMITTER: Curreli F 

PROVIDER: S-EPMC9784924 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature