Screening of the NIH Clinical Collection for inhibitors of HIV-1 integrase activity
Drug repurposing offers a validated approach to reduce drug attrition within the drug discovery and development pipeline through the application of known drugs and drug candidates to treat new indications.
Shaakira Abrahams+4 more
doaj +1 more source
Molecular Epidemiology of HIV-1 in Eastern Europe and Russia
The HIV epidemic in Eastern Europe and Russia is large and not well-controlled. To describe the more recent molecular epidemiology of HIV-1, transmitted drug resistance, and the relationship between the epidemics in this region, we sequenced the protease
Maarten A. A. van de Klundert+19 more
doaj +1 more source
Evaluation of HIV-DNA and inflammatory markers in HIV-infected individuals with different viral load patterns [PDF]
Background: Persistent residual viremia (RV) and low grade inflammation and immune activation have been associated with non-AIDS defining events. The impact of persistent RV and HIV-DNA load on immune activation/ inflammation remains unclear.
Antonelli, Guido+11 more
core +2 more sources
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 ...
Daria J Hazuda
doaj +1 more source
Incorporation of aptamers in the terminal loop of shRNAs yields an effective and novel combinatorial targeting strategy. [PDF]
Gene therapy by engineering patient's own blood cells to confer HIV resistance can potentially lead to a functional cure for AIDS. Toward this goal, we have previously developed an anti-HIV lentivirus vector that deploys a combination of shRNA, ribozyme ...
Castanotto, Daniela+4 more
core +1 more source
Dolutegravir interactions with HIV-1 integrase-DNA: structural rationale for drug resistance and dissociation kinetics. [PDF]
Signature HIV-1 integrase mutations associated with clinical raltegravir resistance involve 1 of 3 primary genetic pathways, Y143C/R, Q148H/K/R and N155H, the latter 2 of which confer cross-resistance to elvitegravir. In accord with clinical findings, in
Felix DeAnda+6 more
doaj +1 more source
Islatravir‐loaded dissolving microarray patches (MAPs) provide a minimally invasive, long‐acting solution for HIV‐1 prevention and treatment. In rats, sustained islatravir delivery lasts up to three months, while in minipigs, efficacious plasma levels are detected for six days.
Qonita Kurnia Anjani+11 more
wiley +1 more source
Persistence of latent, replication-competent Human Immunodeficiency Virus type 1 (HIV-1) provirus is the main impediment towards a cure for HIV/AIDS (Acquired Immune Deficiency Syndrome). Therefore, different therapeutic strategies to eliminate the viral
Lenard S. Vranckx+12 more
doaj +1 more source
Characterization of HIV-1 Integrase Reactions with Viral DNA [PDF]
HIV-1 integrase (integrase) catalyzes the insertion of viral DNA into human chromosomes and is a focus for development of anti-integrase inhibitors to combat HIV infection. Integrase catalyzes two steps, a DNA-end cleavage reaction (3’-processing), and a
Kettlewell, Joanna
core +1 more source
Histone H2AX Is Phosphorylated at Sites of Retroviral DNA Integration but Is Dispensable for Postintegration Repair [PDF]
The histone variant H2AX is rapidly phosphorylated (denoted {gamma}H2AX) in large chromatin domains (foci) flanking double strand DNA (dsDNA) breaks that are produced by ionizing radiation or genotoxic agents and during V(D)J recombination.
Bonner, William+8 more
core +1 more source