, 2021 Previously used as part of salvage therapy, integrase strand transfer inhibitors (INSTIs) have become part of the preferred antiretroviral therapy (ART) first-line regimen in most low- to middle-income countries. With the extensive use of dolutegravir in
Manasa, Justen +7 more
core +1 more source
Resistance to inhibitors of the human immunodeficiency virus type 1 integration
Brazilian Journal of Infectious Diseases, 2010 This review will summarize the role of integrase in HIV-1 infection, the mechanism of integrase inhibitors and resistance with an emphasis on raltegravir (RAL), the first integrase inhibitor licensed to treat HIV-1 infection.
Daria J. Hazuda, PhD
doaj +1 more source
Modeling the HIV-1 Intasome: A Prototype View of the Target of Integrase Inhibitors
Viruses, 2010 The HIV-1 integrase enzyme is essential for integrating the viral DNA into the host chromosome. Infection is aborted in the absence of integration, making integrase an attractive antiviral target. Recently approved inhibitors of integrase bind tightly to
Robert Craigie, Zhiqi Yin
doaj +1 more source
Dialysis purification of integrase-DNA complexes provides high-resolution atomic force microscopy images: dimeric recombinant HIV-1 integrase binding and specific looping on DNA. [PDF]
PLoS ONE, 2013 It remains difficult to obtain high-resolution atomic force microscopy images of HIV-1 integrase bound to DNA in a dimeric or tetrameric fashion. We therefore constructed specific target DNAs to assess HIV-1 integrase binding and purified the complex by ...
Tatsuaki Tsuruyama +5 more
doaj +1 more source
Comparative biochemical analysis of HIV-1 subtype B and C integrase enzymes
Retrovirology, 2009 Background Integrase inhibitors are currently being incorporated into highly active antiretroviral therapy (HAART). Due to high HIV variability, integrase inhibitor efficacy must be evaluated against a range of integrase enzymes from different subtypes ...
Kuhl Björn D +7 more
doaj +1 more source
The Molecular Biology of HIV Integrase [PDF]
Future Virology, 2012 Integration of viral DNA into cellular DNA is an essential step in the replication cycle of HIV and other retroviruses. The first antiviral drugs that target integrase, the viral enzyme that catalyzes DNA integration, have recently been approved and more are in the pipeline. These drugs bind to an intermediate in DNA integration called the intasome, in
openaire +2 more sources
The first total synthesis of lamellarin α 20-sulfate, a selective inhibitor of HIV-1 integrase [PDF]
, 2006 The first total synthesis of lamellarin α 20-sulfate (1), a selective inhibitor of HIV-1 integrase, has been completed. The lamellarin α core in which 13-OH and 20-OH were differentially protected by isopropyl and benzyl groups, respectively, was ...
Iwao, Masatomo +3 more
core +1 more source
, 2019 A series of 5,6,7,8-tetrahydro-1,6-naphthyridine derivatives targeting the allosteric lens-epithelium-derived-growth-factor-p75 (LEDGF/p75)-binding site on HIV-1 integrase, an attractive target for antiviral chemotherapy, was prepared and screened for ...
Timothy Connolly (1754563) +20 more
core +2 more sources
Human immunodeficiency virus : 25 years of diagnostic and therapeutic strategies and their impact on hepatitis B and C virus [PDF]
, 2009 The human immunodeficiency virus (HIV) had spread unrecognized in the human population as sexually transmitted disease and was finally identified by its disease AIDS in 1981.
Hans Wilhelm Doerr +5 more
core +1 more source
Biochemical and virological analysis of the 18-residue C-terminal tail of HIV-1 integrase
Retrovirology, 2009 Background The 18 residue tail abutting the SH3 fold that comprises the heart of the C-terminal domain is the only part of HIV-1 integrase yet to be visualized by structural biology.
Di Nunzio Francesca +6 more
doaj +1 more source