HIV-1 Integrase and ALLINI Structure.
A. Domain Map of HIV-1 Integrase. B. The preclinical lead ALLINI BI-224436. Chemical features common to the ALLINI class are highlighted, including a carboxylic acid moiety (salmon), a tert-butoxy moiety (green), and a large hydrophobic appendage at the ...
Audrey Allen (9324850) +8 more
core +1 more source
Resistance to inhibitors of the human immunodeficiency virus type 1 integration
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
Integration of the proviral DNA intermediate into the host cell genome normally represents an essential step in the retroviral life cycle. While the reason(s) for this requirement remains unclear, it is known that unintegrated proviral DNA is ...
Ishak D. Irwan +4 more
doaj +1 more source
Three main mutational pathways in HIV-2 lead to high-level raltegravir and elvitegravir resistance: implications for emerging HIV-2 treatment regimens. [PDF]
Human immunodeficiency virus type 2 (HIV-2) is intrinsically resistant to non-nucleoside reverse transcriptase inhibitors and exhibits reduced susceptibility to several of the protease inhibitors used for antiretroviral therapy of HIV-1. Thus, there is a
Robert A Smith +10 more
doaj +1 more source
Molecular monitoring of HIV-1 drug resistance in Ifakara HIV-1 Cohort, Tanzania [PDF]
HIV-1 resistance is one of the problems affecting success of antiretroviral therapy programmes worldwide. Many studies on efficacy of ART programmes, specifically on drug resistance, have been conducted in developed countries but not in developing ...
Masimba, Pax Jessey
core +1 more source
Modeling the HIV-1 Intasome: A Prototype View of the Target of Integrase Inhibitors
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
HIV-1 resistance towards integrase inhibitors is a potential threat of the success of HIV-1 combination treatment. G118R is a rare drug resistance mutation conferring pan-integrase resistance.
Helene Mens +3 more
doaj +1 more source
Characterization of natural polymorphic sites of the HIV‐1 integrase before the introduction of HIV‐1 integrase inhibitors in Germany [PDF]
IntroductionThe aim of our study was to analyze the occurrence and evolution of HIV‐1 integrase polymorphisms during the HIV‐1 epidemic in Germany prior to the introduction of the first integrase inhibitor raltegravir in 2007.Materials and MethodsPlasma samples from drug‐naïve HIV‐1 infected individuals newly diagnosed between 1986 and 2006 were used ...
Meixenberger, Karolin +6 more
openaire +3 more sources
Novel machine learning approach toward classification model of HIV-1 integrase inhibitors. [PDF]
HIV-1 (Human immunodeficiency virus-1) has been causing severe pandemics by attacking the immune system of its host. Left untreated, it can lead to AIDS (acquired immunodeficiency syndrome), where death is inevitable due to opportunistic diseases ...
Phan TL +6 more
europepmc +4 more sources
Identification and Optimization of a Novel HIV-1 Integrase Inhibitor. [PDF]
Human immunodeficiency virus-1 (HIV-1) is the causative agent of acquired immunodeficiency syndrome (AIDS). HIV-1, like all retroviruses, stably integrates its vDNA copy into host chromatin, a process allowing for permanent infection. This essential step for HIV-1 replication is catalyzed by viral integrase (IN) and aided by cellular protein LEDGF/p75.
Adu-Ampratwum D +9 more
europepmc +4 more sources

