A biochemical/biophysical assay dyad for HTS-Compatible triaging of inhibitors of the HIV-1 Nef/Hck SH3 Interaction
S. Breuer, S. Espinola, X. Morelli, B.E. Torbett, S.T. Arold, I.H. Engels
Current Chemical Genomics and Translational Medicine, 7:16-20, (2013)
HIV, HTS, Label-free technology, Nef, Protein-protein interaction inhibitor, Resonant waveguide grating, SH3, TR-FRET
The current treatment regimens for HIV include over 20 anti-retrovirals.
However, adverse drug effects and the emergence of drug resistance
necessitates the continued improvement of the existing drug classes as
well as the development of novel drugs that target as yet
therapeutically unexploited viral and cellular pathways. Here we
demonstrate a strategy for the discovery of protein-protein interaction
inhibitors of the viral pathogenicity factor HIV-1 Nef and its
interaction with the host factor SH3. A combination of a time-resolved
fluorescence resonance energy resonance energy transfer-based assay and a
label-free resonant waveguide grating-based assay was optimized for
high-throughput screening formats.
See all publications 2013