Clinical use of HIV integrase inhibitors: a systematic review and meta-analysis. [PDF]
BackgroundOptimal regimen choice of antiretroviral therapy is essential to achieve long-term clinical success. Integrase inhibitors have swiftly been adopted as part of current antiretroviral regimens. The purpose of this study was to review the evidence
Peter Messiaen+5 more
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HIV Dynamics and Integrase Inhibitors [PDF]
The integrase inhibitor (INI) raltegravir has shown promising results in clinical trials to date, reducing second phase HIV RNA levels by 70% in comparison with standard regimens. These trial results have been limited by the 50 copies/ml detection limit of the HIV RNA assay and have not investigated the effect of an INI regimen on levels of latently ...
John M. Murray
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Allosteric Integrase Inhibitor Influences on HIV-1 Integration and Roles of LEDGF/p75 and HDGFL2 Host Factors [PDF]
Allosteric integrase (IN) inhibitors (ALLINIs), which are promising preclinical compounds that engage the lens epithelium-derived growth factor (LEDGF)/p75 binding site on IN, can inhibit different aspects of human immunodeficiency virus 1 (HIV-1 ...
Parmit Kumar Singh+5 more
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Pharmacology of HIV integrase inhibitors [PDF]
The purpose of this paper is to review recent and relevant pharmacology data for three HIV integrase inhibitors: raltegravir (marketed), dolutegravir and elvitegravir (both in Phase III drug development).
Jessica Adams+2 more
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The structural and mechanistic bases for the viral resistance to allosteric HIV-1 integrase inhibitor pirmitegravir [PDF]
Allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) are investigational antiretroviral agents that potently impair virion maturation by inducing hyper-multimerization of IN and inhibiting its interaction with viral genomic RNA. The pyrrolopyridine-based
Tung Dinh+14 more
doaj +3 more sources
Investigation of furo[2,3-h]- and pyridazino[3,4-f]cinnolin-3-ol scaffolds as substrates for the development of novel HIV-1 integrase inhibitors [PDF]
With the aim to develop novel HIV-1 integrase inhibitors, we obtained a set of condensed ring systems based on the furo[2,3-h]cinnolin-3(2H)-one and pyridazino[3,4-f]cinnolin-3-ol scaffolds bearing a potential chelating pharmacophore, which can be ...
Casule, Paola+7 more
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Pre-Treatment Integrase Inhibitor Resistance and Natural Polymorphisms among HIV-1 Subtype C Infected Patients in Ethiopia [PDF]
Dolutegravir-based antiretroviral therapy (ART) has been scaled up in many developing countries, including Ethiopia. However, subtype-dependent polymorphic differences might influence the occurrence of HIV-drug-resistance mutations (HIVDRMs). We analyzed
Dawit Assefa Arimide+7 more
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Antiviral combination therapies consisting of reverse transcriptase inhibitors, protease inhibitors and an integrase inhibitor, have been developed to suppress HIV below the limit of detection.
Dimitra Bon+3 more
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HIV/HCV-coinfection: which role can new antiretrovirals such as integrase inhibitors play? [PDF]
End-stage liver disease has become one of the most frequent causes of death in HIV/HCV-coinfected patients. The role of new antiretrovirals in the progression of liver fibrosis has yet to be defined.
Vogel Martin, Nelson Mark
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Patterns of resistance development with integrase inhibitors in HIV
Raltegravir, the only integrase (IN) inhibitor approved for use in HIV therapy, has recently been licensed. Raltegravir inhibits HIV-1 replication by blocking the IN strand transfer reaction. More than 30 mutations have been associated with resistance to raltegravir and other IN strand transfer inhibitors (INSTIs).
P Cane, Jean L. Mbisa, Martín
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