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The clinical pharmacology of integrase inhibitors

Expert Review of Clinical Pharmacology, 2018
Introduction: Treatment of HIV infection has consistently evolved in the last three decades. A steady improvement in efficacy tolerability, safety, and practical aspects of treatment intake has made HIV infection much easier to manage over the long term, and in optimal treatment conditions the life expectancy of persons living with HIV infection now ...
Di Perri, Giovanni   +3 more
openaire   +2 more sources

Oligomerization of Retrovirus Integrases

2018
Integration of the reverse-transcribed viral cDNA into the host's genome is a critical step in the lifecycle of all retroviruses. Retrovirus integration is carried out by integrase (IN), a virus-encoded enzyme that forms an oligomeric 'intasome' complex with both ends of the linear viral DNA to catalyze their concerted insertions into the backbones of ...
Duane P. Grandgenett, Hideki Aihara
openaire   +3 more sources

Comparison of Integrases Identifies Bxb1-GA Mutant as the Most Efficient Site-Specific Integrase System in Mammalian Cells.

ACS Synthetic Biology, 2019
Phage-derived integrases can catalyze irreversible, site-specific integration of transgenic payloads into a chromosomal locus, resulting in mammalian cells that stably express transgenes or circuits of interest.
Barbara Jusiak   +8 more
semanticscholar   +1 more source

Review of Synthetic Routes and Final Forms of Integrase Inhibitors Dolutegravir, Cabotegravir, and Bictegravir

Organic Process Research & Development, 2019
Bictegravir and dolutegravir are two recently approved integrase inhibitors for the treatment of HIV. A third inhibitor, cabotegravir, is in Phase 3 development.
D. Hughes
semanticscholar   +1 more source

Novel integrase inhibitors for HIV

Expert Opinion on Investigational Drugs, 2010
Integrase inhibitors are the newest class of antiretroviral agents developed to treat HIV-1 infection. Raltegravir (RAL), the only integrase inhibitor (INI) currently approved for the treatment of HIV-infected patients, has proven to be a potent and well-tolerated antiretroviral (ARV) agent.
Martin Markowitz, Nicole Prada
openaire   +3 more sources

Tolerability of HIV integrase inhibitors

Current Opinion in HIV and AIDS, 2012
This review discusses the available safety data for three integrase strand transfer inhibitors (INSTIs)--raltegravir, elvitegravir and dolutegravir--derived from studies in both HIV-infected and HIV-uninfected cohorts.Phase 2 and 3 clinical trials show that all three INSTIs are well tolerated in treatment-naive and treatment-experienced patients with ...
Frederick J. Lee, Andrew Carr
openaire   +2 more sources

Phage Integrases: Biology and Applications

Journal of Molecular Biology, 2004
Phage integrases are enzymes that mediate unidirectional site-specific recombination between two DNA recognition sequences, the phage attachment site, attP, and the bacterial attachment site, attB. Integrases may be grouped into two major families, the tyrosine recombinases and the serine recombinases, based on their mode of catalysis.
Amy C. Groth, Michele P. Calos
openaire   +3 more sources

Zinc binding by retroviral integrase

Biochemical and Biophysical Research Communications, 1992
Zinc binding by integrase from Moloney murine leukaemia virus and a protein A fusion protein containing integrase from human immunodeficiency virus type 1 was demonstrated by a zinc blotting technique using 65ZnCl2. Autoradiography revealed a clear band that was absent from the appropriate controls.
D.W. Hough   +7 more
openaire   +3 more sources

Substrate Recognition by Retroviral Integrases

1999
Substrate recognition by the retroviral IN enzyme is critical for retroviral integration. To catalyze this recombination event, IN must recognize and act on two types of substrates, viral DNA and host DNA, yet the necessary interactions exhibit markedly different degrees of specificity.
Richard A. Katz, Michael Katzman
openaire   +3 more sources

Targeting HIV-1 integrase

Expert Opinion on Therapeutic Targets, 2001
Human immunodeficiency virus Type 1 (HIV-1) integrase is an essential enzyme for the obligatory integration of the viral DNA into the infected cell chromosome. As no cellular homologue of HIV integrase has been identified, this unique HIV-1 enzyme is an attractive target for the development of new therapeutics.
Jocelyn Yelle   +2 more
openaire   +3 more sources

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