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

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

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Article

Authors

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

Engels, Ingo H

KAUST Department

Biological and Environmental Sciences and Engineering (BESE) Division
Bioscience Program
Computational Bioscience Research Center (CBRC)
Structural Biology and Engineering

Date

2013-07-26

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http://hdl.handle.net/10754/334597

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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.

Citation

Breuer S (2013) A Biochemical/Biophysical Assay Dyad for HTS-Compatible Triaging of Inhibitors of the HIV-1 Nef/Hck SH3 Interaction. Current Chemical Genomics and Translational Medicine 7: 16-20. doi:10.2174/2213988501307010016.

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Except where otherwise noted, this item's license is described as This is an open access article licensed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/3.0/) which permits unrestricted, non-commercial use, distribution and reproduction in any medium, provided the work is properly cited.