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

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 vir...

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Autores principales: Breuer, Sebastian, Espinola, Sheryll, Morelli, Xavier, Torbett, Bruce E, Arold, Stefan T, Engels, Ingo H
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Bentham Open 2013
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3854662/
https://www.ncbi.nlm.nih.gov/pubmed/24396731
http://dx.doi.org/10.2174/2213988501307010016
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author Breuer, Sebastian
Espinola, Sheryll
Morelli, Xavier
Torbett, Bruce E
Arold, Stefan T
Engels, Ingo H
author_facet Breuer, Sebastian
Espinola, Sheryll
Morelli, Xavier
Torbett, Bruce E
Arold, Stefan T
Engels, Ingo H
author_sort Breuer, Sebastian
collection PubMed
description 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.
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spelling pubmed-38546622014-01-06 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 Curr Chem Genom Transl Med Article 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. Bentham Open 2013-07-26 /pmc/articles/PMC3854662/ /pubmed/24396731 http://dx.doi.org/10.2174/2213988501307010016 Text en © Breuer et al.; Licensee Bentham Open. http://creativecommons.org/licenses/by-nc/3.0/ 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.
spellingShingle Article
Breuer, Sebastian
Espinola, Sheryll
Morelli, Xavier
Torbett, Bruce E
Arold, Stefan T
Engels, Ingo H
A Biochemical/Biophysical Assay Dyad for HTS-Compatible Triaging of Inhibitors of the HIV-1 Nef/Hck SH3 Interaction
title A Biochemical/Biophysical Assay Dyad for HTS-Compatible Triaging of Inhibitors of the HIV-1 Nef/Hck SH3 Interaction
title_full A Biochemical/Biophysical Assay Dyad for HTS-Compatible Triaging of Inhibitors of the HIV-1 Nef/Hck SH3 Interaction
title_fullStr A Biochemical/Biophysical Assay Dyad for HTS-Compatible Triaging of Inhibitors of the HIV-1 Nef/Hck SH3 Interaction
title_full_unstemmed A Biochemical/Biophysical Assay Dyad for HTS-Compatible Triaging of Inhibitors of the HIV-1 Nef/Hck SH3 Interaction
title_short A Biochemical/Biophysical Assay Dyad for HTS-Compatible Triaging of Inhibitors of the HIV-1 Nef/Hck SH3 Interaction
title_sort biochemical/biophysical assay dyad for hts-compatible triaging of inhibitors of the hiv-1 nef/hck sh3 interaction
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3854662/
https://www.ncbi.nlm.nih.gov/pubmed/24396731
http://dx.doi.org/10.2174/2213988501307010016
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