Toward Structurally Novel and Metabolically Stable HIV-1 Capsid-Targeting Small Molecules.

ABSTRACT: HIV-1 capsid protein (CA) plays an important role in many steps of viral replication and represents an appealing antiviral target. Several CA-targeting small molecules of various chemotypes have been studied, but the peptidomimetic PF74 has drawn particular interest due to its potent antiviral activity, well-characterized binding mode, and unique mechanism of action. Importantly, PF74 competes against important host factors for binding, conferring highly desirable antiviral phenotypes. However, further development of PF74 is hindered by its prohibitively poor metabolic stability, which necessitates the search for structurally novel and metabolically stable chemotypes. We have conducted a pharmacophore-based shape similarity search for compounds mimicking PF74. W

SUBMITTER: Vernekar SKV 

PROVIDER: S-EPMC7232165 | biostudies-literature | 2020 Apr

REPOSITORIES: biostudies-literature