RT inhibitors
MOLECULAR DOCKING STUDIES AND ADME PREDICTION OF NOVEL ISATIN ANALOGS AS HIV 1 RT INHIBITORS WITH BROAD SPECTRUM CHEMO THERAPEUTIC PROPERTIES
... (RT) inhibitors have been discovered to date. The first category of inhibitors is the nucleoside/nucleotide RT inhibitors (NRTIs), which bind to the enzymatic site of RT in a ...
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HIV-1 reverse transcriptase mutations that confer decreased in vitro susceptibility to anti-RT DNA aptamer RT1t49 confer cross resistance to other anti-RT aptamers but not to standard RT inhibitors
... HIV-1 RT with substitutions N255D or N265D that display resistance to the DNA aptamer ...HIV-1 RT variants containing the N255D, N265D or both (Dbl) were tested for the extent of their cross-resistance to ...
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Divergent Evolution in Reverse Transcriptase (RT) of HIV-1 Group O and M Lineages: Impact on Structure, Fitness, and Sensitivity to Nonnucleoside RT Inhibitors
... of RT and linked to other signature ...impact RT activity or function. Group O RT structural models, based on group M subtype B RT crystal structures, revealed that most evolutionarily linked ...
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MOLECULAR DOCKING STUDIES OF NOVEL IMIDAZOLE ANALOGS AS HIV 1 RT INHIBITORS
... . Recent studies also point to the interplay between the NRTI and NNRTI binding sites, possibly explaining the synergies between the two classes of RT inhibitors. Nevirapine (NNRTI) was one of the first ...
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Virtual Screening of Novel HIV RT Inhibitors using Zinc Database
... makes RT a prime target for anti–HIV–therapy, two main categories of HIV RT inhibitors have been discovered to ...of inhibitors is nucleoside analogues ...of inhibitors is nonnucleoside ...
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Two Coselected Distal Mutations in HIV-1 Reverse Transcriptase (RT) Alter Susceptibility to Nonnucleoside RT Inhibitors and Nucleoside Analogs
... active RT in virions led to hypersusceptibility of HIV-1 to azidothymidine (AZT), but not 2,3-dideoxy-3- thiacytidine (3TC), and that the results were likely due to the ability of RT to excise AZT ...mature ...
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Potent Inhibition of Human Immunodeficiency Virus Type 1 Replication by Template Analog Reverse Transcriptase Inhibitors Derived by SELEX (Systematic Evolution of Ligands by Exponential Enrichment)
... analog RT inhibitors (NRTI) bind to the deoxynucleoside triphosphate-binding pocket, which is formed partly by the template-primer nucleic acid and partly by the protein surfaces ...nonnucleoside RT ...
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Inhibition of human endogenous retrovirus K by antiretroviral drugs
... of RT inhibitors on HERV-K infection, we generated HERV-K viral particles with VSV-G pseudotype to facilitate infection of HERV-K in HeLa ...HIV-1 RT was used as equiv- alent of HERV-K RT to ...
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Analysis of 454 sequencing error rate, error sources, and artifact recombination for detection of Low frequency drug resistance mutations in HIV 1 DNA
... to RT inhibitors, we investigated the frequency and mechanisms of point errors, indels, PCR- introduced recombination, and the sensitivity for detect- ing drug resistance mutations in three independent ...
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Differential Sensitivities of Retroviruses to Integrase Strand Transfer Inhibitors
... (RT) inhibitors such as nevirapine are highly selective for HIV-1 (50), whereas the nucleoside RT inhibitor (NRTI) azidothymidine (AZT) inhibits infection by a variety of vi- ruses, including the ...
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Viral resistance to human immunodeficiency virus type 1-specific pyridinone reverse transcriptase inhibitors.
... 4887 Downloaded from http://jvi.asm.org/ on November 10, 2019 by guest Human immunodeficiency virus type 1 HIV-1-specific pyridinone reverse transcriptase RT inhibitors prevent HIV-1 rep[r] ...
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In Vitro Characterization of a Simian Immunodeficiency Virus-Human Immunodeficiency Virus (HIV) Chimera Expressing HIV Type 1 Reverse Transcriptase To Study Antiviral Resistance in Pigtail Macaques
... Prolonged use of RT inhibitors may lead to the appearance of resistant virus. Common mutations leading to NNRTI resis- tance include K103N, Y181C, and Y188C (40), which contribute to the failure of ...
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VIRTUAL SCREENING OF NOVEL HIV RT NNRT INHIBITORS USING ZINC DATABASE
... of RT whereas it contains the active sites of the ...of RT inhibitors, are using clinically, among that which bind directly to polymerase active site nucleoside inhibitors(NRTIs) and ...
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Resistance pattern of human immunodeficiency virus type 1 reverse transcriptase to quinoxaline S-2720.
... Indeed, the quinoxaline derivative has broad-spectrum activity against various mutant HIV-1 strains that are resistant to other HIV-1-specific RT inhibitors; i.e., quinoxaline S-2720 is [r] ...
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1 Amino 6 chloro 2 (1H pyrrol 2 yl)benzimidazole (RS 1350)
... many RT inhibitors were synthesized and some were selected as lead compounds for clinical trials (Artico, 1996; Pedersen et ...of RT inhibitors were identified (Vandamme et ...competitive ...
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TNF-α induces matrix metalloproteinase-9-dependent soluble intercellular adhesion molecule-1 release via TRAF2-mediated MAPKs and NF-κB activation in osteoblast-like MC3T3-E1 cells
... Results: We applied gelatin zymography, Western blot, RT-PCR, real-time PCR, selective pharmacological inhibitors of transcription (actinomycin D, Act.D), translation (cycloheximide, CHI[r] ...
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Therapeutic Potential of Small Molecule MicroRNA Inhibition.
... In previous research in the Deiters lab, miRNA-21 (miR-21) was selected as a target, because it is highly upregulated in many human malignancies including cancer. Elevated miR-21 expression was demonstrated in breast, ...
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RT-SHIV, an infectious CCR5-tropic chimeric virus suitable for evaluating HIV reverse transcriptase inhibitors in macaque models
... single dose of 30 mg) for 30 days prior to virus challenge to minimize animal susceptibility variation by synchro- nizing their reproductive cycles. Another group of four macaques were not pretreated with DMPA prior to ...
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New Developments in Quantitative Real-time Polymerase Chain Reaction Technology
... The first step towards analysing microbial gene expression requires a quantitative extraction of RNA. This step has proven to be highly problematic for environmental matrices, due to compounded inefficiencies in ...
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Per-residue energy decomposition pharmacophore model to enhance virtual screening in drug discovery: a study for identification of reverse transcriptase inhibitors as potential anti-HIV agents
... our proposed approach, we applied the same docking pro- cedure to a set of experimentally determined inhibitors with known HIV-1 RT inhibition activity. In our approach, we intend to unshackle the ...
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