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| Verfasst von: | Machara, Aleš [VerfasserIn]  |
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| | Lux, Vanda [VerfasserIn] |
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| | Kožíšek, Milan [VerfasserIn] |
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| | Grantz Šašková, Klára [VerfasserIn] |
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| | Štěpánek, Ondřej [VerfasserIn] |
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| | Kotora, Martin [VerfasserIn] |
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| | Parkan, Kamil [VerfasserIn] |
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| | Pávová, Marcela [VerfasserIn] |
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| | Glass, Bärbel [VerfasserIn] |
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| | Sehr, Peter [VerfasserIn] |
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| | Lewis, Joe [VerfasserIn] |
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| | Müller, Barbara [VerfasserIn] |
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| | Kräusslich, Hans-Georg [VerfasserIn] |
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| | Konvalinka, Jan [VerfasserIn] |
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| Titel: | Specific inhibitors of HIV capsid assembly binding to the c-terminal domain of the capsid protein |
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| Titelzusatz: | evaluation of 2-arylquinazolines as potential antiviral compounds |
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| Verf.angabe: | 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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| Jahr: | 2016 |
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| Jahr des Originals: | 2015 |
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| Umfang: | 14 S. |
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| Fussnoten: | Publication date December 21, 2015 ; Gesehen am 22.05.2020 |
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| Titel Quelle: | Enthalten in: Journal of medicinal chemistry |
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| Ort Quelle: | Washington, DC : ACS, 1959 |
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| Jahr Quelle: | 2016 |
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| Band/Heft Quelle: | 59(2016), 2, Seite 545-558 |
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| ISSN Quelle: | 1520-4804 |
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| Abstract: | 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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| DOI: | doi:10.1021/acs.jmedchem.5b01089 |
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| URL: | Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.
Volltext: https://doi.org/10.1021/acs.jmedchem.5b01089 |
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| | DOI: https://doi.org/10.1021/acs.jmedchem.5b01089 |
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| Datenträger: | Online-Ressource |
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| Sprache: | eng |
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| K10plus-PPN: | 1698687249 |
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| Verknüpfungen: | → Zeitschrift |
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Specific inhibitors of HIV capsid assembly binding to the c-terminal domain of the capsid protein / Machara, Aleš [VerfasserIn]; 2016 (Online-Ressource)
