Brujita Integrase: A Simple, Arm-Less, Directionless, and Promiscuous Tyrosine Integrase System
نویسندگان
چکیده
منابع مشابه
Integrase illuminated.
The long struggle to develop effective therapies against human immunodeficiency virus (HIV) continues in earn est. New antiretroviral drugs to prevent integration of the viral genome are undergoing clinical trials. However, the drug development has relied on testing for effectiveness with only limited understanding of the structural aspects of HIV integration. To establish successful infection,...
متن کاملResistance to Integrase Inhibitors
Integrase (IN) is a clinically validated target for the treatment of human immunodeficiency virus infections and raltegravir exhibits remarkable clinical activity. The next most advanced IN inhibitor is elvitegravir. However, mutant viruses lead to treatment failure and mutations within the IN coding sequence appear to confer cross-resistance. The characterization of those mutations is critical...
متن کاملStyrylquinolines, integrase inhibitors acting prior to integration: a new mechanism of action for anti-integrase agents.
We have previously shown that styrylquinolines (SQLs) are integrase inhibitors in vitro. They compete with the long terminal repeat substrate for integrase. Here, we describe the cellular mode of action of these molecules. We show that SQLs do not interfere with virus entry. In fact, concentrations of up to 20 times the 50% inhibitory concentration did not inhibit cell-to-cell fusion or affect ...
متن کاملCatalytically-active complex of HIV-1 integrase with a viral DNA substrate binds anti-integrase drugs.
HIV-1 integration into the host cell genome is a multistep process catalyzed by the virally-encoded integrase (IN) protein. In view of the difficulty of obtaining a stable DNA-bound IN at high concentration as required for structure determination, we selected IN-DNA complexes that form disulfide linkages between 5'-thiolated DNA and several single mutations to cysteine around the catalytic site...
متن کاملNatural polymorphism of the HIV-1 integrase gene and mutations associated with integrase inhibitor resistance.
BACKGROUND Two inhibitors of the HIV-1 integrase enzyme (INIs) are in late stage clinical development. To date, approximately 42 mutations within the HIV-1 integrase (IN) gene have been associated with INI drug resistance. Naturally occurring IN gene polymorphisms may have important implications for INI development. In this study, we evaluated clinical HIV-1 strains from INI-naive patients to d...
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ژورنال
عنوان ژورنال: Journal of Molecular Biology
سال: 2016
ISSN: 0022-2836
DOI: 10.1016/j.jmb.2016.04.023