A Mos1 transposase in vivo assay to screen new HIV-1 integrase inhibitors
Sign Up to like & getrecommendations! Published in 2018 at "Genetica"
DOI: 10.1007/s10709-018-0007-1
Abstract: The integrase and transposase enzymes of retrovirus and transposons, respectively, share the catalytic DDE domain. In vitro assays showed that inhibitors of HIV-1 integrase generally inhibit the mariner Mos1 transposase. Using a Drosophila strain in… read more here.
Keywords: integrase; mos1 transposase; transposase vivo; transposase ... See more keywords
Pharmacokinetics of HIV-Integrase Inhibitors During Pregnancy: Mechanisms, Clinical Implications and Knowledge Gaps
Sign Up to like & getrecommendations! Published in 2018 at "Clinical Pharmacokinetics"
DOI: 10.1007/s40262-018-0684-z
Abstract: Prevention of mother-to-child transmission of HIV and optimal maternal treatment are the most important goals of antiretroviral therapy in pregnant women with HIV. These goals may be at risk due to possible reduced exposure during… read more here.
Keywords: integrase inhibitors; pharmacokinetics hiv; pregnant women; inhibitors pregnancy ... See more keywords
The inhibition process of HIV-1 integrase by diketoacids molecules: Understanding the factors governing the better efficiency of dolutegravir.
Sign Up to like & getrecommendations! Published in 2017 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2017.05.001
Abstract: The Human Immunodeficiency Virus-1 integrase is responsible for the covalent insertion of a newly synthesized double-stranded viral DNA into the host cells, and is an emerging target for antivirus drug design. Raltegravir (RAL) and elvitegravir… read more here.
Keywords: integrase; process hiv; inhibition process; hiv integrase ... See more keywords
HIV integrase inhibitors that inhibit strand transfer interact with RAG1 and hamper its activities.
Sign Up to like & getrecommendations! Published in 2021 at "International immunopharmacology"
DOI: 10.1016/j.intimp.2021.107515
Abstract: Multiple steps of the retroviral infection process have been targeted over the years to develop therapeutic approaches, starting from the entry of the virus into the cell till the viral DNA integration to host genome.… read more here.
Keywords: integrase inhibitors; inhibit strand; inhibitors inhibit; strand transfer ... See more keywords
Allosteric HIV integrase inhibitors promote formation of inactive branched polymers via homomeric carboxy-terminal domain interactions.
Sign Up to like & getrecommendations! Published in 2020 at "Structure"
DOI: 10.1016/j.str.2020.12.001
Abstract: The major effect of allosteric HIV integrase (IN) inhibitors (ALLINIs) is observed during virion maturation, where ALLINI treatment interrupts IN-RNA interactions via drug-induced IN aggregation, leading to the formation of aberrant virions. To understand the… read more here.
Keywords: integrase inhibitors; carboxy terminal; formation; homomeric carboxy ... See more keywords
Design, Synthesis, and Preclinical Profiling of GSK3739936 (BMS-986180), an Allosteric Inhibitor of HIV-1 Integrase with Broad-Spectrum Activity toward 124/125 Polymorphs.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c02169
Abstract: Allosteric HIV-1 integrase inhibitors (ALLINIs) have garnered special interest because of their novel mechanism of action: they inhibit HIV-1 replication by promoting aberrant integrase multimerization, leading to the production of replication-deficient viral particles. The binding… read more here.
Keywords: design synthesis; integrase; hiv integrase; 125 polymorphs ... See more keywords
Treatment of HIV Infections with HIV Integrase Inhibitors.
Sign Up to like & getrecommendations! Published in 2017 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.6b00456
Abstract: Human immunodeficiency virus (HIV) infections and related diseases remain as major public health problems worldwide. The replication of HIV type 1 (HIV-1) requires the actions of three essential enzymes: reverse transcriptase, protease, and integrase. There… read more here.
Keywords: integrase inhibitors; infections hiv; hiv infections; hiv ... See more keywords
Synthesis of C3,C6-Diaryl 7-Azaindoles via One-Pot Suzuki–Miyaura Cross-Coupling Reaction and Evaluation of Their HIV-1 Integrase Inhibitory Activity
Sign Up to like & getrecommendations! Published in 2023 at "ACS Omega"
DOI: 10.1021/acsomega.2c07372
Abstract: There is a continuing demand of new inhibitors of HIV-1 Integrase (HIV-1 IN) due to mutations of HIV-1. This study aims to develop the synthesis of 3,6-diaryl 7-azaindoles and introspect the role of aryl groups… read more here.
Keywords: diaryl azaindoles; synthesis; synthesis diaryl; one pot ... See more keywords
Structural biology: High-order integration
Sign Up to like & getrecommendations! Published in 2017 at "Nature Reviews Microbiology"
DOI: 10.1038/nrmicro.2017.3
Abstract: To establish a lasting infection, lentiviruses, such as HIV-1, stably integrate their DNA into the chromatin of host cells. Integration is mediated by the viral integrase enzyme in a multimeric nucleoprotein complex called the intasome,… read more here.
Keywords: integrase; order; integration; dna ... See more keywords
Biochemical activity of RAGs is impeded by Dolutegravir, an HIV integrase inhibitor.
Sign Up to like & getrecommendations! Published in 2020 at "Cell death discovery"
DOI: 10.1038/s41420-020-0281-4
Abstract: HIV is a retrovirus that infects CD4+ T lymphocytes in human beings and causes immunodeficiency. In the recent years, various therapies have been developed against HIV, including targeting the HIV specific protein, integrase, responsible for… read more here.
Keywords: integrase; inhibitors elvitegravir; hiv; integrase inhibitor ... See more keywords
GCN2 phosphorylates HIV-1 integrase and decreases HIV-1 replication by limiting viral integration
Sign Up to like & getrecommendations! Published in 2017 at "Scientific Reports"
DOI: 10.1038/s41598-017-02276-0
Abstract: GCN2 is a serine/threonine kinase involved in cellular stress response related to amino acid starvation. Previously, we showed that GCN2 interacts with HIV-1 integrase and is activated during HIV-1 infection. Herein, we identified HIV-1 integrase… read more here.
Keywords: integrase; integration; gcn2; gcn2 phosphorylates ... See more keywords