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Showing 1 to 20 of 56 for “"integrase"”.
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Characterization of IntDOT, the CTnDOT Integrase
Sequence analysis revealed that the integrase of the Bacteroides conjugative transposon CTnDOT (IntDOT) might be a member of the tyrosine recombinase family because IntDOT has five of six highly conserved residues found in the catalytic domains of tyrosine recombinases. Yet, IntDOT catalyzes a …
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Design and synthesis of HIV-1 integrase inhibitors
In recent years, HIV-1 integrase (IN) has emerged as an attractive target for the treatment of human immunodeficiency virus type 1 (HIV-1), the causative pathogen of acquired immuno-deficiency syndrome (AIDS). Several classes of IN inhibitors are known but many of these compounds are toxic, do not …
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Structure-function analysis of IntDOT, the CTnDOT integrase
IntDOT is an enzyme required for the recombination reactions that promote movement of CTnDOT that is an integrative conjugative element (ICE) found in Bacteroides spp. IntDOT has been classified in the tyrosine recombinase family. However, unlike most other tyrosine recombinases that require …
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Impact of integrase inhibitors on gut and oral microbiome
La infección por el virus de la inmunodeficiencia humana (VIH) es considerada actualmente como una enfermedad crónica gracias al uso del tratamiento antirretroviral (TAR). Sin embargo, a pesar del TAR, estos pacientes pueden presentar un estado de inmunoactivación e inflamación crónica, así como un …
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Synthesis and Computational Studies on Hiv-1 Integrase Inhibitors
HIV-1 integrase (IN) is essential for viral replication and offers a promising target for the development of anti-retroviral drugs. Two decades of extensive research has lead to the recent approval of raltegravir as the first IN inhibitor. Advancement of drug candidate elvitegravir, which is …
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Characterization of the Integrase of the Bacteroides Mobilizable Transposon NBU1
… Bacteroides mobilizable transposon NBU1 uses an integrase (IntN1) for its integration and excision from the host chromosome. IntN1 has six conserved amino acids in the C-terminal end (RKHRHY) that are characteristic of tyrosine recombinases. I used site-directed mutagenesis to construct alanine …
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A genetic analysis of bacteriophage lambda integrase-core site interactions
… chromosome during lysogeny. The viral protein, Integrase (Int), catalyzes strand exchange between the phage attachment site, attP, and the host target sequence, attB to generate the prophage sites, attL and attR. attP contains the core region, where strand exchange occurs, and the required …
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Genetic and mechanistic studies of the bacteriophage lambda integrase protein
… a series of steps catalyzed by the phage-encoded integrase (Int). In order to study the functions of Int during recombination, Int mutants defective in in vivo excision were isolated and screened for proficiency in binding to the arm-type sites using challenge phage assays. Fifty-eight such …
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Coordination and Catalysis of the Lambda Integrase Site -Specific Recombination Reaction
… the maximal cleavage and ligation activity of Integrase. From this work, we concluded that para-Nitrophenol tyrosine analogs are optimal for quantitative in vitro measurement of Int ligation. Int could not utilize tyrosine analogs para-Cresol and dimethyl- p-phenylenediamine as ligation …
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Mutational analysis of integrase and excisionase proteins in bacteriophage lambda site-specific recombination system
Second-site reversion analyses were performed on 21 recombination defective Int mutants. A second-site revertant P243L/E218K and a pseudorevertant E175K were isolated and further characterized using genetic and biochemical methods. The results showed that the second-site substitution E218K …
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Genetic analysis of lambda integrase and Escherichia coli integration host factor: Interactions with their recognition sites
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Characterizing interactions between the cellular HIV-1 integration cofactor, LEDGF/p75 with chromatin and HIV-1 integrase
… genome into its host genome. The viral enzyme integrase (IN) catalyzes 3’-viral cDNA processing and DNA strand transfer reactions leading to the integration of the viral cDNA into the host DNA. HIV-1 IN is a promising therapeutic target due to the lack of a cellular counterpart. The first …
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The Role of Specific Integrase Strand Transfer Inhibitors (INSTIs) in the Alteration of Oligodendrocyte Maturation and Myelination in Hand
… HIV patients recommends anew class of drugs, the integrasestrand transferinhibitors(INSTIs)as front-line therapy, we examined if two specific INSTIs, Elvitegravir (EVG) and raltegravir (RAL), altered the survival and/or maturation of developing oligodendrocytes in vitroand in vivo. We found that …
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Dissecting the Contribution of the Carboxyl-Terminal Domain and Tail of HIV-1 Integrase to Viral Dynamics and Enzymatic Function
… new class of antiviral drugs targeting the viral integrase (IN) has been added to the HAART (high active antiretroviral therapy) regimen. This novel drug class exerts its inhibitory effect by targeting one aspect of the dual-staged integration reaction. In contrast to the other two viral targets …
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Repurposing the human immunodeficiency virus (HIV) integrase inhibitor raltegravir for the treatment of felid alphaherpesvirus 1 (FHV-1) ocular infection
… is a human immunodeficiency virus (HIV) integrase inhibitor that was recently shown to poses antiviral activity against human herpesviruses. Then, electric cell-substrate impedance sensing (ECIS) was evaluated as a novel methodology to study the replication kinetics of herpesviruses. It …
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Bacteroides Conjugative Transposons: Ecology and Mechanisms
… had shown that the attDOT recombination site and integrase of CTnDOT (IntDOT) are sufficient and essential for integration in vivo. Even though the integrase of CTnDOT belongs to the lambda integrase family of recombinases, the mechanism of integration of CTnDOT is different from that of phage …
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Biochemical, Structural, And Drug Design Studies Of Multi-Drug Resistant Hiv-1 Therapeutic Targets
… to multi-drug resistance to HIV-1 protease and integrase inhibitors. </p> <p>Proper proteolytic processing of the HIV-1 Gag/Pol polyprotein is required for HIV infection and viral replication. This feature has made HIV-1 protease an attractive target for antiretroviral drug design for the …
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Exploring the Early Events in the HIV-1 Life Cycle: From Post-Entry Restriction to Nuclear Import
… that is present in incoming virions, HIV-1 integrase, is an enzyme that facilitates the fusion of the viral genome and the host genomic DNA in the nucleus, thereby making HIV a permanent fixture in infected individuals. We have discovered that, in addition to its role in catalyzing …
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A study of clinical strains of Pseudomonas Aeruginosa and the investigation of antibiotic resistance mechanisms in the multidrug resistant strain PA13
… BLASTN analysis identified these as being an integrase gene (ORF1), an aminoglycoside acetyltransferase gene, aac(6’)-Ib (ORF2), an oxacillinase gene (ORF3) and a quaternary ammonium compound resistance gene (ORF4). The presence of the integrase gene and the quaternary ammonium compound gene …
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Bioinformatic analysis: Retroposon sequences containing multiple putative endonucleases
… endonuclease functions include a retroviral-like integrase (IN), an apurinic-apyrimidinic endonuclease (APE), the PDD endonuclease recently identified in the R2BM retroposon and an HNH endonuclease signature conserved by the group 11 intron sequences. The results indicate that the spliced l eader …
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