期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 59, 期 2, 页码 545-558出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.5b01089
关键词
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资金
- Grant Agency of the Czech Republic [13-19561S]
- seventh Framework Program of the EU [FP7-HEALTH-201095]
- Chemical Biology Core Facility (CBCF) at the European Molecular Biology Laboratory (EMBL)
- German Cancer Research Centre (DKFZ)
- University of Heidelberg
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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