A Biochemical/Biophysical Assay Dyad for HTS-Compatible Triaging of Inhibitors of the HIV-1 Nef/Hck SH3 Interaction

Sebastian Breuer, Sheryll Espinola, Xavier Morelli, Bruce E Torbett, Stefan T. Arold, Ingo H Engels

Research output: Contribution to journalArticlepeer-review

Abstract

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.
Original languageEnglish (US)
Pages (from-to)16-20
Number of pages5
JournalCurrent Chemical Genomics and Translational Medicine
Volume7
DOIs
StatePublished - Jul 26 2013

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