Kirsch, Philine; Jakob, Valentin; Oberhausen, Kevin; Stein, Saskia C.; Cucarro, Ivano; Schulz, Thomas F.; Empting, Martin published the artcile< Fragment-Based Discovery of a Qualified Hit Targeting the Latency-Associated Nuclear Antigen of the Oncogenic Kaposi's Sarcoma-Associated Herpesvirus/Human Herpesvirus 8>, Formula: C9H8O, the main research area is Kaposi sarcoma human herpesvirus 8 antiviral LANA.
The latency-associated nuclear antigen (LANA) is required for latent replication and persistence of Kaposi’s sarcoma-associated herpesvirus/human herpesvirus 8. It acts via replicating and tethering the virus episome to the host chromatin and exerts other functions. We conceived a new approach for the discovery of antiviral drugs to inhibit the interaction between LANA and the viral genome. We applied a biophys. screening cascade and identified the first LANA binders from small, structurally diverse compound libraries. Starting from a fragment-sized scaffold, we generated optimized hits via fragment growing using a dedicated fluorescence-polarization-based assay as the structure-activity-relationship driver. We improved compound potency to the double-digit micromolar range. Importantly, we qualified the resulting hit through orthogonal methods employing EMSA, STD-NMR, and MST methodologies. This optimized hit provides an ideal starting point for subsequent hit-to-lead campaigns providing evident target-binding, suitable ligand efficiencies, and favorable physicochem. properties.
Journal of Medicinal Chemistry published new progress about Antiviral agents. 10602-04-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C9H8O, Formula: C9H8O.
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts