Articles with "integrase" as a keyword



Multipart DNA Assembly Using Site-Specific Recombinases from the Large Serine Integrase Family.

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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

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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

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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
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The inhibition process of HIV-1 integrase by diketoacids molecules: Understanding the factors governing the better efficiency of dolutegravir.

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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.

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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

N-Substituted Bicyclic Carbamoyl Pyridones: Integrase Strand Transfer Inhibitors that Potently Inhibit Drug-Resistant HIV-1 Integrase Mutants

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Published in 2024 at "ACS Infectious Diseases"

DOI: 10.1021/acsinfecdis.3c00525

Abstract: HIV-1 integrase (IN) is an important molecular target for the development of anti-AIDS drugs. A recently FDA-approved second-generation integrase strand transfer inhibitor (INSTI) cabotegravir (CAB, 2021) is being marketed for use in long-duration antiviral formulations.… read more here.

Keywords: integrase; cab; integrase strand; potently inhibit ... See more keywords

Discovery and Preclinical Profiling of GSK3839919, a Potent HIV-1 Allosteric Integrase Inhibitor.

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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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Published in 2022 at "ACS Omega"

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

A Hot-Swappable Genetic Switch: Building an Inducible and Trackable Functional Assay for the Essential Gene MEDIATOR 21.

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Published in 2025 at "ACS synthetic biology"

DOI: 10.1021/acssynbio.5c00085

Abstract: Essential genes, estimated to be approximately 20% of the Arabidopsis genome, are broadly expressed and required for reproductive success. They are difficult to study, as interfering with their function leads to premature death. Transcription is… read more here.

Keywords: integrase; med21; mediator; expression ... See more keywords

Structural biology: High-order integration

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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
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Biochemical activity of RAGs is impeded by Dolutegravir, an HIV integrase inhibitor.

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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