Probing Resistance Mutations in Retroviral Integrases by Direct Measurement of Dolutegravir Fluorescence

FDA-approved integrase strand transfer inhibitors (raltegravir, elvitegravir and dolutegravir) efficiently inhibit HIV-1 replication. Here, we present fluorescence properties of these inhibitors. Dolutegravir displays an excitation mode particularly dependent on Mg 2+ chelation, allowing to directly probe its Mg 2+ -dependent binding to the prototype foamy virus (PFV) integrase. Dolutegravir-binding studied by both its fluorescence anisotropy...