Results 41 to 50 of about 30,382,849 (226)

HIV-1 Integrase Inhibitors

open access: yesDrugs in R & D, 2007
From the discovery of HIV-1 integrase (IN) inhibitors using enzyme-based assays in 1992, it has taken 15 years to achieve success in human clinical trials. Currently available antiretroviral drugs set high clinical standards in efficacy and long-term safety for upcoming novel HIV/AIDS therapeutic agents.
Raveendra, Dayam   +2 more
openaire   +2 more sources

Human immunodeficiency virus : 25 years of diagnostic and therapeutic strategies and their impact on hepatitis B and C virus [PDF]

open access: yes, 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

No difference in HIV-1 integrase resistance between CSF and blood compartments Short title: HIV-1 integrase resistance in compartments

open access: yes, 2021
International audienceBackground: Little is known about the HIV-1 integrase resistance in CNS. This study aimed to evaluate integrase resistance in CSF, as a marker of CNS, and compare it to the HIV resistance in plasma.
Simon, Anne   +13 more
core   +1 more source

CoMFA and CoMSIA Studies on Inhibitors of HIV-1 Integrase - Bicyclic Pyrimidinones

open access: yesE-Journal of Chemistry, 2010
To understand the structural requirements of HIV-1 integrase inhibitors and to design new ligands against human HIV-1 integrase with enhanced inhibitory potency, a 3D QSAR (quantitative structure-activity relationship) study with comparative molecular ...
V. Radhika, S. Sree Kanth, M. Vijjulatha
doaj   +1 more source

INSTIs and NNRTIs Potently Inhibit HIV-1 Polypurine Tract Mutants in a Single Round Infection Assay

open access: yesViruses, 2021
Integrase strand transfer inhibitors (INSTIs) are a class of antiretroviral compounds that prevent the insertion of a DNA copy of the viral genome into the host genome by targeting the viral enzyme integrase (IN).
Steven J. Smith   +6 more
doaj   +1 more source

Allosteric inhibition of HIV-1 integrase activity [PDF]

open access: yesCurrent Opinion in Chemical Biology, 2013
HIV-1 integrase is an important therapeutic target in the fight against HIV/AIDS. Integrase strand transfer inhibitors (INSTIs), which target the enzyme active site, have witnessed clinical success over the past 5 years, but the generation of drug resistance poses challenges to INSTI-based therapies moving forward.
Alan, Engelman   +2 more
openaire   +2 more sources

Uneven Genetic Robustness of HIV-1 Integrase [PDF]

open access: yesJournal of Virology, 2015
ABSTRACT Genetic robustness (tolerance of mutation) may be a naturally selected property in some viruses, because it should enhance adaptability. Robustness should be especially beneficial to viruses like HIV-1 that exhibit high mutation rates and exist in immunologically hostile environments.
Suzannah J, Rihn   +3 more
openaire   +2 more sources

Resistance to inhibitors of the human immunodeficiency virus type 1 integration

open access: yesBrazilian Journal of Infectious Diseases
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

Characterization of HIV-1 integrase interaction with human Ku70 protein and initial implications for drug targeting

open access: yesScientific Reports, 2017
Human Ku70/Ku80 protein is known to influence HIV-1 replication. One of the possible reasons may be the protection of integrase from proteasomal degradation by Ku70 subunit. We demonstrated that recombinant HIV-1 integrase and Ku70 form a stable complex,
Andrey N. Anisenko   +6 more
doaj   +1 more source

Docking and Molecular Dynamics Calculations of Some Previously Studied and newly Designed Ligands to Catalytic Core Domain of HIV-1 Integrase and an Investigation to Effects of Conformational Changes of Protein on Docking Results

open access: yesJournal of the Turkish Chemical Society, Section A: Chemistry, 2016
Nowadays, AIDS still remains as a worldwide pandemic and continues to cause many death which arise from HIV-1 virus. For nearly 35 years, drugs that target various steps of virus life cycle have been developed.
Selami Ercan
doaj   +1 more source

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