Development of an AlphaScreen-Based HIV-1 Integrase Dimerization Assay for Discovery of Novel Allosteric Inhibitors

In recent years, HIV-1 integrase (IN) has become an established target in the field of antiretroviral drug discovery. However, its sole clinically approved inhibitor, the integrase strand transfer inhibitor (INSTI) raltegravir, has a surprisingly low genetic barrier for resistance. Furthermore, the...

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Veröffentlicht in:	Journal of biomolecular screening 2012-06, Vol.17 (5), p.618-628
Hauptverfasser:	Demeulemeester, Jonas, Tintori, Cristina, Botta, Maurizio, Debyser, Zeger, Christ, Frauke
Format:	Artikel
Sprache:	eng
Schlagworte:	Allosteric properties Allosteric Regulation - drug effects Antiviral agents Clinical trials Cross-resistance Drug discovery Enzyme Assays - methods high-throughput screening High-Throughput Screening Assays - methods HIV Integrase - chemistry HIV Integrase - metabolism HIV Integrase Inhibitors - pharmacology Human immunodeficiency virus 1 Humans Integrase Protein Multimerization - drug effects Quality Control Recombinant Fusion Proteins - chemistry Recombinant Fusion Proteins - metabolism Reproducibility of Results Sensitivity and Specificity
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