Multipart DNA Assembly Using Site-Specific Recombinases from the Large Serine Integrase Family.
Sign Up to like & getrecommendations! Published in 2017 at "Methods in molecular biology"
DOI: 10.1007/978-1-4939-7169-5_19
Abstract: Assembling multiple DNA fragments into functional plasmids is an important and often rate-limiting step in engineering new functions in living systems. Bacteriophage integrases are enzymes that carry out efficient recombination reactions between short, defined DNA sequences… read more here.
Keywords: integrase; assembly using; dna; serine integrase ... See more keywords
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
Novel secondary mutations C56S and G149A confer resistance to HIV‐1 integrase strand transfer inhibitors
Sign Up to like & getrecommendations! Published in 2018 at "Antiviral Research"
DOI: 10.1016/j.antiviral.2018.01.013
Abstract: ABSTRACT Cabotegravir (CAB, S/GSK1265744) is an investigational second‐generation integrase strand transfer inhibitor (INSTI) with a chemical structure similar to dolutegravir. CAB is under development as a long‐acting injectable formulation for treatment of HIV‐1 infection and… read more here.
Keywords: integrase; c56s g149a; strand transfer; resistance ... 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
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
Discovery and Preclinical Profiling of GSK3839919, a Potent HIV-1 Allosteric Integrase Inhibitor.
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.2c00115
Abstract: Allosteric HIV-1 integrase inhibitors (ALLINIs) have been of interest recently because of their novel mechanism of action. Strategic modifications to the C5 moiety of a class of 4-(4,4-dimethylpiperidinyl)-2,6-dimethylpyridinyl ALLINIs led to the identification of a… read more here.
Keywords: toxicology; hiv; preclinical profiling; integrase ... See more keywords
Identification and Optimization of a Novel HIV-1 Integrase Inhibitor
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DOI: 10.1021/acsomega.1c06378
Abstract: 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… read more here.
Keywords: optimization novel; hiv; integrase; identification optimization ... 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
High prevalence of integrase mutation L74I in West African HIV-1 subtypes prior to integrase inhibitor treatment
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Antimicrobial Chemotherapy"
DOI: 10.1093/jac/dkaa033
Abstract: Abstract Objectives HIV-1 integrase inhibitors are recommended as first-line therapy by WHO, though efficacy and resistance data for non-B subtypes are limited. Two recent trials have identified the integrase L74I mutation to be associated with… read more here.
Keywords: integrase; hiv; prevalence; resistance ... See more keywords