Results 221 to 230 of about 28,079 (244)
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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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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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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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HIV integrase inhibitors: a new era in the treatment of HIV
Expert Opinion on Pharmacotherapy, 2015Integrase inhibitors (INIs) are the latest class of antiretroviral drugs approved for the treatment of HIV infection and are becoming 'standard' drugs in the treatment of both naïve as well as heavily pretreated individuals with HIV.Data on efficacy, safety, tolerability, pharmacokinetics, drug-drug interactions and resistance are reviewed from the ...
Ana Milinkovic+3 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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Practical Synthesis of a HIV Integrase Inhibitor
Organic Process Research & Development, 2008A practical and efficient synthesis of the potent HIV integrase inhibitor 1 is described. Starting from readily available 3,4-dihydro-2H-pyran, the six-step synthesis features a through process without purification of any of the intermediates until the isolation of crystalline intermediate 7.
David A. Conlon+14 more
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Hydrazide-Containing Inhibitors of HIV-1 Integrase
Journal of Medicinal Chemistry, 1997Inhibitors of HIV integrase are currently being sought as potential new therapeutics for the treatment of AIDS. A large number of inhibitors discovered to date contain the o-bis-hydroxy catechol structure. In an effort to discover structural leads for the development of new HIV integrase inhibitors which do not rely on this potentially cytotoxic ...
George W. A. Milne+7 more
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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 inhibitors as therapeutic agents in AIDS
Reviews in Medical Virology, 2007AbstractHIV‐1 integrase is a protein of Mr 32 000 encoded at the 3′‐end of the pol gene. Integration of HIV DNA into the host cell chromosomal DNA apparently occurs by a carefully defined sequence of DNA tailoring (3′‐processing (3′P)) and coupling (integration) reactions.
Vasu Nair, Guochen Chi
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Integrase Inhibitors Against HIV: Efficacy and Resistance
Future Virology, 2016Divisione Clinicizzata di Malattie Infettive, Dipartimento di Scienze Biomediche e Cliniche ‘Luigi Sacco’, Universita degli Studi di Milano, via G.B. Grassi 74, 20157 Milano, Italy *Author for correspondence: Tel.: +39 02 5031 9761; Fax: +39 02 5031 9758; stefano.rusconi@unimi ...
P. Tau, S. Rusconi
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