Results 201 to 210 of about 22,886 (216)
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Raltegravir: The first HIV integrase inhibitor
Clinical Therapeutics, 2008The availability of new classes of antiretroviral drugs has made it possible for HIV-infected individuals who are highly treatment experienced to achieve the goals of immunologic recovery and virologic suppression. Raltegravir is the first integrase inhibitor to be approved by the US Food and Drug Administration for use in antiretroviral treatment ...
Betty J. Dong, Jennifer Cocohoba
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HIV integrase as a target for antiviral chemotherapy
Reviews in Medical Virology, 2002AbstractOne of the three key enzymes encoded by the pol gene of HIV is a Mr 32 000 protein called HIV integrase. This viral enzyme is involved in the integration of HIV DNA into host chromosomal DNA. There appears to be no functional equivalent of the enzyme in human cells.
Vasu Nair, Vasu Nair
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The future of integrase inhibitors of HIV-1
Current Opinion in Virology, 2012Integration of the HIV-1 DNA is required and essential to maintain the viral DNA in the infected cell. Integration process occurs in several events, mainly endonucleolytic processing of the 3' ends of the viral DNA and strand transfer or joining of the viral and cellular DNA.
Anne-Geneviève Marcelin+2 more
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Structure and Function of HIV-1 Integrase
Current Topics in Medicinal Chemistry, 2004HIV-1 integrase is a multidomain enzyme which is required for the integration of viral DNA into the host genome. It is one of three enzymes of HIV, the others being the Reverse Transcriptase and the Protease. It is an attractive target for therapeutic drug design. The enzyme consists of three domains.
David R. Davies, Thang K Chiu
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HIV integrase: a target for drug discovery
Genes and Function, 1997Current antiviral strategies against HIV rely on structure–function analysis of HIV reverse transcriptase (RT) and protease (PR). The third viral pol gene product, HIV integrase (IN), is also a good target for drug discovery, since IN is essential for retroviral replication and, moreover, it has no obvious functional analogue in the host.
Ramon A. Puras Lutzke+1 more
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Dolutegravir, an HIV integrase inhibitor for the treatment of HIV infection
Drugs of Today, 2014Dolutegravir, a next-generation integrase strand transfer inhibitor, was recently approved by the United States Food and Drug Administration to treat antiretroviral therapy-naive as well as treatment-experienced HIV-infected individuals, including those who have been treated with other integrase strand transfer inhibitors.
Zelalem Temesgen+2 more
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Journal of the American Academy of Physician Assistants, 2016
Integrase strand transfer inhibitors (INSTIs) are a class of antiretroviral agents used to treat HIV. These drugs--raltegravir, elvitegravir, and dolutegravir--are preferred options for treatment-naïve patients when used in combination with two nucleoside reverse transcriptase inhibitors.
Nathan Trustman+2 more
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Integrase strand transfer inhibitors (INSTIs) are a class of antiretroviral agents used to treat HIV. These drugs--raltegravir, elvitegravir, and dolutegravir--are preferred options for treatment-naïve patients when used in combination with two nucleoside reverse transcriptase inhibitors.
Nathan Trustman+2 more
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The HIV integrase catalytic core
Nature Structural & Molecular Biology, 1995The structure of the catalytic domain of HIV integrase reveals a similarity with other proteins involved in DNA recombination or RNA degradation. Knowledge of the structure may help in the search for inhibitors of HIV replication.
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Quinoline-based HIV Integrase Inhibitors
Current Pharmaceutical Design, 2013HIV integrase became an important target for drug development more than twenty years ago. However, progress has been hampered by the lack of assays suitable for high throughput screening, a reliable crystal structure or pharmacophore. Thus, a real breakthrough was only observed in 2007 with the introduction of the first integrase inhibitor, raltegravir,
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Hiv integrase: a target for aids therapeutics
Trends in Biotechnology, 1997HIV integrase catalyses the incorporation of virally derived DNA into the human genome. This unique step in the virus life cycle provides a variety of points for intervention and hence is an attractive target for the development of new therapeutics for the treatment of AIDS.
Thomas, Mark, Brady, Leo
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