Specific inhibitors of HIV capsid assembly binding to the c-terminal domain of the capsid protein: evaluation of 2-arylquinazolines as potential antiviral compounds
Assembly of human immunodeficiency virus (HIV-1) represents an attractive target for antiretroviral therapy which is not exploited by currently available drugs. We established high-throughput screening for assembly inhibitors based on competition of small molecules for the binding of a known dodecap...
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| Hauptverfasser: | , , , , , , , , , , , , , |
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| Dokumenttyp: | Article (Journal) |
| Sprache: | Englisch |
| Veröffentlicht: |
2016
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| In: |
Journal of medicinal chemistry
Year: 2015, Jahrgang: 59, Heft: 2, Pages: 545-558 |
| ISSN: | 1520-4804 |
| DOI: | 10.1021/acs.jmedchem.5b01089 |
| Online-Zugang: | Verlag, lizenzpflichtig, Volltext: https://doi.org/10.1021/acs.jmedchem.5b01089
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| Verfasserangaben: | Aleš Machara, Vanda Lux, Milan Kožíšek, Klára Grantz Šašková, Ondřej Štěpánek, Martin Kotora, Kamil Parkan, Marcela Pávová, Bärbel Glass, Peter Sehr, Joe Lewis, Barbara Müller, Hans-Georg Kräusslich, and Jan Konvalinka |
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| 245 | 1 | 0 | |a Specific inhibitors of HIV capsid assembly binding to the c-terminal domain of the capsid protein |b evaluation of 2-arylquinazolines as potential antiviral compounds |c Aleš Machara, Vanda Lux, Milan Kožíšek, Klára Grantz Šašková, Ondřej Štěpánek, Martin Kotora, Kamil Parkan, Marcela Pávová, Bärbel Glass, Peter Sehr, Joe Lewis, Barbara Müller, Hans-Georg Kräusslich, and Jan Konvalinka |
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| 520 | |a Assembly of human immunodeficiency virus (HIV-1) represents an attractive target for antiretroviral therapy which is not exploited by currently available drugs. We established high-throughput screening for assembly inhibitors based on competition of small molecules for the binding of a known dodecapeptide assembly inhibitor to the C-terminal domain of HIV-1 CA (capsid). Screening of >70000 compounds from different libraries identified 2-arylquinazolines as low micromolecular inhibitors of HIV-1 capsid assembly. We prepared focused libraries of modified 2-arylquinazolines and tested their capacity to bind HIV-1 CA to compete with the known peptide inhibitor and to prevent the replication of HIV-1 in tissue culture. Some of the compounds showed potent binding to the C-terminal domain of CA and were found to block viral replication at low micromolar concentrations. | ||
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