Reverse Transcriptase Inhibitors
HIV Reverse Transcriptase
A reverse transcriptase encoded by the POL GENE of HIV. It is a heterodimer of 66 kDa and 51 kDa subunits that are derived from a common precursor protein. The heterodimer also includes an RNAse H activity (RIBONUCLEASE H, HUMAN IMMUNODEFICIENCY VIRUS) that plays an essential role the viral replication process.
Anti-HIV Agents
Drug Resistance, Viral
HIV-1
Nevirapine
HIV Infections
Zidovudine
A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.
Delavirdine
HIV Protease Inhibitors
RNA-Directed DNA Polymerase
Organophosphonates
Stavudine
Dideoxynucleosides
Nucleosides that have two hydroxy groups removed from the sugar moiety. The majority of these compounds have broad-spectrum antiretroviral activity due to their action as antimetabolites. The nucleosides are phosphorylated intracellularly to their 5'-triphosphates and act as chain-terminating inhibitors of viral reverse transcription.
Drug Resistance, Multiple, Viral
Didanosine
A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. Didanosine is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase; ddI is then metabolized to dideoxyadenosine triphosphate, its putative active metabolite.
Antiretroviral Therapy, Highly Active
Lamivudine
Nucleosides
Ritonavir
Zalcitabine
A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication at low concentrations, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal toxic side effect is axonal degeneration resulting in peripheral neuropathy.
Lopinavir
Viral Load
HIV
Human immunodeficiency virus. A non-taxonomic and historical term referring to any of two species, specifically HIV-1 and/or HIV-2. Prior to 1986, this was called human T-lymphotropic virus type III/lymphadenopathy-associated virus (HTLV-III/LAV). From 1986-1990, it was an official species called HIV. Since 1991, HIV was no longer considered an official species name; the two species were designated HIV-1 and HIV-2.
CD4 Lymphocyte Count
Drug Therapy, Combination
Mutation
Treatment Failure
Virus Replication
HIV Protease
Nelfinavir
Ribonuclease H
HIV Integrase Inhibitors
HIV-Associated Lipodystrophy Syndrome
Telomerase
Reverse Transcriptase Polymerase Chain Reaction
Antiviral Agents
Agents used in the prophylaxis or therapy of VIRUS DISEASES. Some of the ways they may act include preventing viral replication by inhibiting viral DNA polymerase; binding to specific cell-surface receptors and inhibiting viral penetration or uncoating; inhibiting viral protein synthesis; or blocking late stages of virus assembly.
Drug Interactions
Molecular Sequence Data
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
Thymine Nucleotides
Acidosis, Lactic
pol Gene Products, Human Immunodeficiency Virus
Mutation, Missense
Genotype
Furans
HIV-2
An HIV species related to HIV-1 but carrying different antigenic components and with differing nucleic acid composition. It shares serologic reactivity and sequence homology with the simian Lentivirus SIMIAN IMMUNODEFICIENCY VIRUS and infects only T4-lymphocytes expressing the CD4 phenotypic marker.
Saquinavir
Indinavir
Pyrrolidinones
Acquired Immunodeficiency Syndrome
An acquired defect of cellular immunity associated with infection by the human immunodeficiency virus (HIV), a CD4-positive T-lymphocyte count under 200 cells/microliter or less than 14% of total lymphocytes, and increased susceptibility to opportunistic infections and malignant neoplasms. Clinical manifestations also include emaciation (wasting) and dementia. These elements reflect criteria for AIDS as defined by the CDC in 1993.
Base Sequence
Nitriles
Drug Resistance, Microbial
Amino Acid Substitution
The naturally occurring or experimentally induced replacement of one or more AMINO ACIDS in a protein with another. If a functionally equivalent amino acid is substituted, the protein may retain wild-type activity. Substitution may also diminish, enhance, or eliminate protein function. Experimentally induced substitution is often used to study enzyme activities and binding site properties.
Pyridines
Inhibitory Concentration 50
Protease Inhibitors
Lipodystrophy
A collection of heterogenous conditions resulting from defective LIPID METABOLISM and characterized by ADIPOSE TISSUE atrophy. Often there is redistribution of body fat resulting in peripheral fat wasting and central adiposity. They include generalized, localized, congenital, and acquired lipodystrophy.
Foscarnet
Erythrocebus patas
DNA, Mitochondrial
Sulfur Compounds
Area Under Curve
A statistical means of summarizing information from a series of measurements on one individual. It is frequently used in clinical pharmacology where the AUC from serum levels can be interpreted as the total uptake of whatever has been administered. As a plot of the concentration of a drug against time, after a single dose of medicine, producing a standard shape curve, it is a means of comparing the bioavailability of the same drug made by different companies. (From Winslade, Dictionary of Clinical Research, 1992)
Templates, Genetic
Microbial Sensitivity Tests
Drug Design
The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include pharmacokinetics, dosage analysis, or drug administration analysis.
Treatment Outcome
Pyrimidines
Leukocytes, Mononuclear
Deoxyadenosines
Botswana
Molecular Structure
DNA Primers
Cells, Cultured
Sequence Analysis, DNA
Drug Combinations
Polymerase Chain Reaction
In vitro method for producing large amounts of specific DNA or RNA fragments of defined length and sequence from small amounts of short oligonucleotide flanking sequences (primers). The essential steps include thermal denaturation of the double-stranded target molecules, annealing of the primers to their complementary sequences, and extension of the annealed primers by enzymatic synthesis with DNA polymerase. The reaction is efficient, specific, and extremely sensitive. Uses for the reaction include disease diagnosis, detection of difficult-to-isolate pathogens, mutation analysis, genetic testing, DNA sequencing, and analyzing evolutionary relationships.
Chromatography, High Pressure Liquid
Models, Molecular
Amino Acid Sequence
Structure-Activity Relationship
HIV Fusion Inhibitors
Dose-Response Relationship, Drug
Drug Administration Schedule
Drug Evaluation, Preclinical
Cohort Studies
Studies in which subsets of a defined population are identified. These groups may or may not be exposed to factors hypothesized to influence the probability of the occurrence of a particular disease or other outcome. Cohorts are defined populations which, as a whole, are followed in an attempt to determine distinguishing subgroup characteristics.
Mutagenesis, Site-Directed
Infectious Disease Transmission, Vertical
Biotransformation
The chemical alteration of an exogenous substance by or in a biological system. The alteration may inactivate the compound or it may result in the production of an active metabolite of an inactive parent compound. The alterations may be divided into METABOLIC DETOXICATION, PHASE I and METABOLIC DETOXICATION, PHASE II.
RNA
A polynucleotide consisting essentially of chains with a repeating backbone of phosphate and ribose units to which nitrogenous bases are attached. RNA is unique among biological macromolecules in that it can encode genetic information, serve as an abundant structural component of cells, and also possesses catalytic activity. (Rieger et al., Glossary of Genetics: Classical and Molecular, 5th ed)
Plasma
Carbamates
Derivatives of carbamic acid, H2NC(=O)OH. Included under this heading are N-substituted and O-substituted carbamic acids. In general carbamate esters are referred to as urethanes, and polymers that include repeating units of carbamate are referred to as POLYURETHANES. Note however that polyurethanes are derived from the polymerization of ISOCYANATES and the singular term URETHANE refers to the ethyl ester of carbamic acid.
Phenotype
Simian immunodeficiency virus
Organophosphorus Compounds
CD4-Positive T-Lymphocytes
A critical subpopulation of T-lymphocytes involved in the induction of most immunological functions. The HIV virus has selective tropism for the T4 cell which expresses the CD4 phenotypic marker, a receptor for HIV. In fact, the key element in the profound immunosuppression seen in HIV infection is the depletion of this subset of T-lymphocytes.
Gels
Retroelements
Elements that are transcribed into RNA, reverse-transcribed into DNA and then inserted into a new site in the genome. Long terminal repeats (LTRs) similar to those from retroviruses are contained in retrotransposons and retrovirus-like elements. Retroposons, such as LONG INTERSPERSED NUCLEOTIDE ELEMENTS and SHORT INTERSPERSED NUCLEOTIDE ELEMENTS do not contain LTRs.
Administration, Intravaginal
Pregnancy Complications, Infectious
RNA, Messenger
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
Drug Monitoring
Half-Life
Binding Sites
Indoles
Retrospective Studies
Studies used to test etiologic hypotheses in which inferences about an exposure to putative causal factors are derived from data relating to characteristics of persons under study or to events or experiences in their past. The essential feature is that some of the persons under study have the disease or outcome of interest and their characteristics are compared with those of unaffected persons.
HIV Seropositivity
RNA, Transfer, Lys
Moloney murine leukemia virus
Pyrazoles
Genes, pol
Spectrophotometry, Ultraviolet
Drug Resistance, Multiple
Macaca mulatta
Simian Acquired Immunodeficiency Syndrome
South Africa
Mitochondria
Semiautonomous, self-reproducing organelles that occur in the cytoplasm of all cells of most, but not all, eukaryotes. Each mitochondrion is surrounded by a double limiting membrane. The inner membrane is highly invaginated, and its projections are called cristae. Mitochondria are the sites of the reactions of oxidative phosphorylation, which result in the formation of ATP. They contain distinctive RIBOSOMES, transfer RNAs (RNA, TRANSFER); AMINO ACYL T RNA SYNTHETASES; and elongation and termination factors. Mitochondria depend upon genes within the nucleus of the cells in which they reside for many essential messenger RNAs (RNA, MESSENGER). Mitochondria are believed to have arisen from aerobic bacteria that established a symbiotic relationship with primitive protoeukaryotes. (King & Stansfield, A Dictionary of Genetics, 4th ed)
Cytochrome P-450 CYP3A
A cytochrome P-450 suptype that has specificity for a broad variety of lipophilic compounds, including STEROIDS; FATTY ACIDS; and XENOBIOTICS. This enzyme has clinical significance due to its ability to metabolize a diverse array of clinically important drugs such as CYCLOSPORINE; VERAPAMIL; and MIDAZOLAM. This enzyme also catalyzes the N-demethylation of ERYTHROMYCIN.
Prevalence
Prospective Studies
Tandem Mass Spectrometry
A mass spectrometry technique using two (MS/MS) or more mass analyzers. With two in tandem, the precursor ions are mass-selected by a first mass analyzer, and focused into a collision region where they are then fragmented into product ions which are then characterized by a second mass analyzer. A variety of techniques are used to separate the compounds, ionize them, and introduce them to the first mass analyzer. For example, for in GC-MS/MS, GAS CHROMATOGRAPHY-MASS SPECTROMETRY is involved in separating relatively small compounds by GAS CHROMATOGRAPHY prior to injecting them into an ionization chamber for the mass selection.
Avian leukosis virus
Inhibition of human immunodeficiency virus type 1 replication by combination of transcription inhibitor K-12 and other antiretroviral agents in acutely and chronically infected cells. (1/2177)
8-Difluoromethoxy-1-ethyl-6-fluoro-1,4-dihydro-7-[4-(2-methoxyp hen yl)-1- piperazinyl]-4-oxoquinoline-3-carboxylic acid (K-12) has recently been identified as a potent and selective inhibitor of human immunodeficiency virus type 1 (HIV-1) transcription. In this study, we examined several combinations of K-12 and other antiretroviral agents for their inhibitory effects on HIV-1 replication in acutely and chronically infected cell cultures. Combinations of K-12 and a reverse transcriptase (RT) inhibitor, either zidovudine, lamivudine, or nevirapine, synergistically inhibited HIV-1 replication in acutely infected MT-4 cells. The combination of K-12 and the protease inhibitor nelfinavir (NFV) also synergistically inhibited HIV-1, whereas the synergism of this combination was weaker than that of the combinations with the RT inhibitors. K-12 did not enhance the cytotoxicities of RT and protease inhibitors. Synergism of the combinations was also observed in acutely infected peripheral blood mononuclear cells. The combination of K-12 and cepharanthine, a nuclear factor kappa B inhibitor, synergistically inhibited HIV-1 production in tumor necrosis factor alpha-stimulated U1 cells, a promonocytic cell line chronically infected with the virus. In contrast, additive inhibition was observed for the combination of K-12 and NFV. These results indicate that the combinations of K-12 and clinically available antiretroviral agents may have potential as chemotherapeutic modalities for the treatment of HIV-1 infection. (+info)Safety and pharmacokinetics of abacavir (1592U89) following oral administration of escalating single doses in human immunodeficiency virus type 1-infected adults. (2/2177)
Abacavir (1592U89) is a nucleoside analog reverse transcriptase inhibitor that has been demonstrated to have selective activity against human immunodeficiency virus (HIV) in vitro and favorable safety profiles in mice and monkeys. A phase I study was conducted to evaluate the safety and pharmacokinetics of abacavir following oral administration of single escalating doses (100, 300, 600, 900, and 1,200 mg) to HIV-infected adults. In this double-blind, placebo-controlled study, subjects with baseline CD4+ cell counts ranging from < 50 to 713 cells per mm3 (median, 315 cells per mm3) were randomly assigned to receive abacavir (n = 12) or placebo (n = 6). The bioavailability of the caplet formulation relative to that of the oral solution was also assessed with the 300-mg dose. Abacavir was well tolerated by all subjects; mild to moderate asthenia, abdominal pain, headache, diarrhea, and dyspepsia were the most frequently reported adverse events, and these were not dose related. No significant clinical or laboratory abnormalities were observed throughout the study. All doses resulted in mean abacavir concentrations in plasma that exceeded the mean 50% inhibitory concentration (IC50) for clinical HIV isolates in vitro (0.07 microgram/ml) for almost 3 h. Abacavir was rapidly absorbed following oral administration, with the time to the peak concentration in plasma occurring at 1.0 to 1.7 h postdosing. Mean maximum concentrations in plasma (Cmax) and the area under the plasma concentration-time curve from time zero to infinity (AUC0-infinity) increased slightly more than proportionally from 100 to 600 mg (from 0.6 to 4.7 micrograms/ml for Cmax; from 1.0 to 15.7 micrograms.h/ml for AUC0-infinity) but increased proportionally from 600 to 1,200 mg (from 4.7 to 9.6 micrograms/ml for Cmax; from 15.7 to 32.8 micrograms.h/ml for AUC0-infinity. The elimination of abacavir from plasma was rapid, with an apparent elimination half-life of 0.9 to 1.7 h. Abacavir was well absorbed, with a relative bioavailability of the caplet formulation of 96% versus that of an oral solution (drug substance in water). In conclusion, this study showed that abacavir is safe and is well tolerated by HIV-infected subjects and demonstrated predictable pharmacokinetic characteristics when it was administered as single oral doses ranging from 100 to 1,200 mg. (+info)Safety and single-dose pharmacokinetics of abacavir (1592U89) in human immunodeficiency virus type 1-infected children. (3/2177)
Abacavir (formerly 1592U89) is a potent 2'-deoxyguanosine analog reverse transcriptase inhibitor that has been demonstrated to have a favorable safety profile in initial clinical trials with adults with human immunodeficiency virus (HIV) type 1 infection. A phase I study was conducted to evaluate the pharmacokinetics and safety of abacavir following the administration of two single oral doses (4 and 8 mg/kg of body weight) to 22 HIV-infected children ages 3 months to 13 years. Plasma was collected for analysis at predose and at 0.5, 1, 1.5, 2, 2.5, 3, 5, and 8 h after the administration of each dose. Plasma abacavir concentrations were determined by high-performance liquid chromatography, and data were analyzed by noncompartmental methods. Abacavir was well tolerated by all subjects. The single abacavir-related adverse event was rash, which occurred in 2 of 22 subjects. After administration of the oral solution, abacavir was rapidly absorbed, with the time to the peak concentration in plasma occurring within 1.5 h postdosing. Pharmacokinetic parameter estimates were comparable among the different age groups for each dose level. The mean maximum concentration in plasma (Cmax) and the mean area under the curve from time zero to infinity (AUC0-infinity) increased by 16 and 45% more than predicted, respectively, as the abacavir dose was doubled from 4 to 8 mg/kg (Cmax increased from 1.69 to 3.94 micrograms/ml, and AUC0-infinity increased from 2.82 to 8.09 micrograms.h/ml). Abacavir was rapidly eliminated, with a mean elimination half-life of 0.98 to 1.13 h. The mean apparent clearance from plasma decreased from 27.35 to 18.88 ml/min/kg as the dose increased. Neither body surface area nor creatinine clearance were correlated with pharmacokinetic estimates at either dose. The extent of exposure to abacavir appears to be slightly lower in children than in adults, with the comparable unit doses being based on body weight. In conclusion, this study showed that abacavir is safe and well tolerated in children when it is administered as a single oral dose of 4 or 8 mg/kg. (+info)Suppression of replication of multidrug-resistant HIV type 1 variants by combinations of thymidylate synthase inhibitors with zidovudine or stavudine. (4/2177)
The replication of recombinant multidrug-resistant HIV-1 clones modeled on clinically derived resistant HIV-1 strains from patients receiving long-term combination therapy with zidovudine (AZT) plus 2',3'-dideoxycytidine was found to regain sensitivity to AZT and stavudine (D4T) as a consequence of a pharmacologically induced decrease in de novo dTMP synthesis. The host-cell system used was phytohemagglutinin-stimulated peripheral blood mononuclear cells; dTMP and dTTP depletion were induced by single exposures to a low level of the thymidylate synthase inhibitor 5-fluorouracil (5-FU) or its deoxynucleoside, 2'-deoxy-5-fluorouridine. The host-cell response to the latter was biphasic: a very rapid decrease in the rate of de novo dTMP formation and, consequently, in intracellular dTTP pools, followed by slower recovery in both indices over 3 to 24 h. With the additional presence of AZT or D4T, however, replication of the multidrug-resistant HIV-1 strains remained inhibited, indicating dependence of HIV DNA chain termination by AZT-5'-monophosphate or 2',3'-didehydro-2', 3'-dideoxythymidine-5'-monophosphate in these resistant strains on simultaneous inhibition of host-cell de novo synthesis of thymidine nucleotides. No effect on viability of control (uninfected) phytohemagglutinin-stimulated/peripheral blood mononuclear cells was noted on 6-day exposures to 5-FU or 2'-deoxy-5-fluorouridine alone or in combination with AZT or D4T, even at drug levels severalfold higher than those used in the viral inhibition studies. These studies may provide useful information for the potential clinical use of AZT/5-FU or D4T/5-FU combinations for the prevention or reversal of multidrug resistance associated with long-term dideoxynucleoside combination therapy. (+info)Functional analysis of mutations conferring lamivudine resistance on hepatitis B virus. (5/2177)
Two patterns of mutation are commonly observed in the polymerase gene of lamivudine [(-)2'-deoxy-3'-thiacytidine]-resistant hepatitis B virus (HBV). The M539I substitution in the conserved YMDD motif occurs independently of other changes, whereas the M539V substitution is associated with an additional upstream change (L515M). These mutations were introduced into a common background and their effects on HBV DNA replication and lamivudine resistance studied. The L515M and M539V mutations provided only partial resistance while the M539I mutation conferred a high degree of lamivudine resistance. The combination of the L515M and M539V mutations gave an intermediate level of replication competence, compared with either mutation alone, and increased resistance to lamivudine. This probably accounts for these two mutations always being observed together. The M539I mutation reduced replication competence. (+info)The cost-effectiveness of treatment with lamivudine and zidovudine compared with zidovudine alone: a comparison of Markov model and trial data estimates. (6/2177)
In this paper, we present a Markov model for estimating the cost-effectiveness of combination therapy with lamivudine (LMV) and zidovudine (ZDV) compared with ZDV alone. We also compare the predictions of the Markov model for the impact of combination therapy on trial period costs with the actual impact of combination therapy on selected trial period costs estimated from data collected during the clinical trials. In the Markov model, disease stages were defined by CD4 cell count. Based on clinical trial data for patients with CD4 counts higher than 100 cells/mm3, the model assumed that the CD4 cell count level could be maintained above the level at the initiation of therapy for 6.5 months with monotherapy and for 18 months with combination therapy. After this period, transition rates for natural disease progression were used. Incremental lifetime costs and quality-adjusted life years gained with LMV/ZDV compared with ZDV alone were estimated for cohorts of patients initiating antiretroviral therapy at four different CD4 cell count stages. Cost per life year gained varied from $10,000 to $18,000, and cost per quality-adjusted life year gained varied from $14,000 to $27,000. In both cases, the combination therapy was more cost-effective when started earlier in disease progression. These estimates were not sensitive to changes in key parameter values. In addition, the model was used to estimate the impact of combination therapy on healthcare costs during the trial period; these estimated costs were compared with data on the cost of resource use collected during the clinical trial for hospital stays, unscheduled visits, medications, and outpatient procedures. Both the Markov model estimates and the trial data estimates for the trial period showed cost savings in other medical costs, though these were not large enough to completely offset the increased cost for antiretroviral therapy. The model estimates were more conservative than the estimates based on the trial data. (+info)Antiviral effect and pharmacokinetic interaction between nevirapine and indinavir in persons infected with human immunodeficiency virus type 1. (7/2177)
Nevirapine and indinavir have the potential of affecting the pharmacokinetics of each other. In a prospective trial, 24 human immunodeficiency virus (HIV)-infected subjects on stable nucleoside or no therapy were treated with 800 mg of indinavir every 8 h. After 7 days, 200 mg of nevirapine a day was added for 14 days and then increased to 200 mg twice a day. At day 7 (before nevirapine), there was a sevenfold difference among the subjects in indinavir area under the curve (AUC), and there was a significant correlation between indinavir AUC (r2=0.378, P=.019), minimum plasma concentration (Cmin; r2=0.359, P=.023), maximum plasma concentration (Cmax; r2=0.340, P=.028), and plasma HIV RNA decline. Nevirapine significantly reduced median indinavir Cmin (47.5%) and AUC (27.4%) and, to a lesser extent, Cmax (11%). Plasma HIV RNA values were +info)Genotypic resistance and the treatment of HIV-1 infection in Espirito Santo, Brazil. (8/2177)
Before December 1997, in Espirito Santo, Brazil, combination antiretroviral therapy was used without routine virologic or immunologic monitoring. To examine consequences of therapy in this setting, clinical information, human immunodeficiency virus type 1 (HIV-1) RNA levels, CD4 cell counts, and protease and reverse transcriptase sequences were determined for consecutive HIV-1-infected outpatients. Of 48 treatment-naive individuals, 11 were started on therapy for HIV-related symptoms; however, 44 (92%) had an RNA level >20,000 copies/mL, a CD4 cell count <500/mm3, or symptoms. Eighteen (51%) of 35 patients on therapy had an RNA level >20,000 copies/mL. Nucleoside-resistance mutations were observed in 21 (68%) of 31 nucleoside-experienced subjects. Protease mutations necessary for high-level protease inhibitor (PI) resistance were present together with permissive mutations in 3 of 10 PI-experienced patients. Inability to identify high-risk individuals and to detect virologic failure may limit the effectiveness of antiretroviral drug programs and may promote the spread of drug resistance where virologic and immunologic monitoring are not available. (+info)
Nucleoside reverse-transcriptase inhibitor dosing errors in an outpati by James H. Willig, Andrew O. Westfall et al.
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References
Pre-incubation of cell-free HIV-1 group M isolates with non-nucleoside reverse transcriptase inhibitors blocks subsequent viral...
Quantifying the treatment efficacy of reverse transcriptase inhibitors: new analyses of clinical data based on within-host...
Maraviroc and reverse transcriptase inhibitors combinations as potential preexposure prophylaxis candidates - GOV.UK
Prevention of Perinatal Transmission of HIV-1 Without Nucleoside Reverse Transcriptase Inhibitors | Clinical Research Trial...
Prevention of Perinatal Transmission of HIV-1 Without Nucleoside Reverse Transcriptase Inhibitors | Clinical Research Trial...
Racivir | CAS#143491-54-7 | transcriptase inhibitor | MedKoo
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Gilead Sciences and Merck Establish Agreement for Distribution of ATRIPLA(TM) in Developing Countries | Gilead
Prevalence of genotypic HIV-1 drug resistance in Thailand, 2002 | Annals of Clinical Microbiology and Antimicrobials | Full Text
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Anti-viral drug
Isolate Data
Reverse-transcriptase inhibitor
Nucleotide analog reverse-transcriptase inhibitors (NtARTIs or NtRTIs) Non-nucleoside reverse-transcriptase inhibitors (NNRTIs ... Discovery and development of non-nucleoside reverse-transcriptase inhibitors Protease inhibitors Discovery and development of ... Reverse-transcriptase inhibitors (RTIs) are a class of antiretroviral drugs used to treat HIV infection or AIDS, and in some ... Reverse+Transcriptase+Inhibitors at the US National Library of Medicine Medical Subject Headings (MeSH) (Articles with short ...
Discovery and development of non-nucleoside reverse-transcriptase inhibitors
... nucleoside/nucleotide reverse-transcriptase inhibitors (NRTIs/NtRTIs) and non-nucleoside reverse-transcriptase inhibitors ( ... Medicine portal Viruses portal Antiretroviral drug Reverse-transcriptase inhibitor Protease inhibitor Entry inhibitor Discovery ... Non-nucleoside reverse-transcriptase inhibitors (NNRTIs) are antiretroviral drugs used in the treatment of human ... Jochmans D (June 2008). "Novel HIV-1 reverse transcriptase inhibitors". Virus Research. 134 (1-2): 171-85. doi:10.1016/j. ...
Discovery and development of nucleoside and nucleotide reverse-transcriptase inhibitors
... protease inhibitors, entry inhibitors, co-receptor inhibitors and integrase inhibitors. The reverse transcriptase of HIV-1 has ... Nucleoside and nucleotide reverse-transcriptase inhibitors, Non-nucleoside reverse-transcriptase inhibitors, ... development of CCR5 receptor antagonists HIV/AIDS research Reverse-transcriptase inhibitor Protease inhibitor Entry inhibitor ... non-nucleoside reverse-transcriptase inhibitors and protease inhibitors. Currently, there are several NRTIs in various stages ...
Namandjé Bumpus
Bumpus has also researched nonnucleoside reverse transcriptase inhibitors. Her lab was the first to publish the P450-catalyzed ... Nucleotide Reverse Transcriptase Inhibitors". Expert Opinion on Pharmacotherapy. 13 (1): 65-79. doi:10.1517/14656566.2012. ... Tenofovir is a nucleotide analog reverse transcriptase inhibitor that prevents the HIV virus from replicating. Tenofovir is ... rilpivirine and etravirine and was first to characterize the metabolism of the nonnucleoside reverse transcriptase inhibitor ...
Acute fatty liver of pregnancy
Montessori V, Harris M, Montaner JS (2003). "Hepatotoxicity of nucleoside reverse transcriptase inhibitors". Seminars in Liver ... including nucleoside reverse transcriptase inhibitors used to treat HIV, and a rare condition known as Jamaican vomiting ...
Zidovudine
... such as a protease inhibitor, non-nucleoside reverse-transcriptase inhibitor, or integrase inhibitor; this type of therapy is ... ZDV is of the nucleoside analog reverse-transcriptase inhibitor (NRTI) class. It works by inhibiting the enzyme reverse ... Their research efforts were focused in part on the viral enzyme reverse transcriptase. Reverse transcriptase is an enzyme that ... Quan, Y; Rong, L; Liang, C; Wainberg, MA (1999). "Reverse Transcriptase Inhibitors Can Selectively Block the Synthesis of ...
Ofelia Olivero
Olivero, Ofelia A. (April 2007). "Mechanisms of genotoxicity of nucleoside reverse transcriptase inhibitors". Environmental and ...
Elsulfavirine
It is a non-nucleoside reverse transcriptase inhibitor (NNRTI). Elsulfavirine is a prodrug which is metabolized to the active ... Wang Y, De Clercq E, Li G (October 2019). "Current and emerging non-nucleoside reverse transcriptase inhibitors (NNRTIs) for ... Wang Y, De Clercq E, Li G (October 2019). "Current and emerging non-nucleoside reverse transcriptase inhibitors (NNRTIs) for ... Rai MA, Pannek S, Fichtenbaum CJ (June 2018). "Emerging reverse transcriptase inhibitors for HIV-1 infection". Expert Opinion ...
Enzyme inhibitor
... reverse-transcriptase inhibitors targeting HIV/AIDS, neuraminidase inhibitors targeting influenza, and terminase inhibitors ... Li G, Wang Y, De Clercq E (April 2022). "Approved HIV reverse transcriptase inhibitors in the past decade". Acta Pharmaceutica ... For example, an inhibitor might compete with substrate A for the first binding site, but be a non-competitive inhibitor with ... New inhibitors are used to obtain crystallographic structures of the enzyme in an inhibitor/enzyme complex to show how the ...
Abacavir
"Nucleoside reverse transcriptase inhibitors (NRTIs or 'nukes') - HIV/AIDS". www.hiv.va.gov. Archived from the original on 9 ... Abacavir is a nucleoside reverse transcriptase inhibitor that inhibits viral replication. It is a guanosine analogue that is ... Similar to other nucleoside analog reverse-transcriptase inhibitors (NRTIs), abacavir is used together with other HIV ... a Potent Inhibitor of HIV Reverse Transcriptase". The Journal of Organic Chemistry. 61 (13): 4192-4193. doi:10.1021/jo960708p. ...
Portmanteau inhibitor
v t e (Reverse transcriptase inhibitors, Antiretroviral drugs, Integrase inhibitors, All stub articles, Antiinfective agent ... Minnesota researchers who designed and synthesized a combination HIV reverse transcriptase inhibitor and an integrase inhibitor ... "Rationally Designed Dual Inhibitors of HIV Reverse Transcriptase and Integrase". Journal of Medicinal Chemistry. 50 (15): 3416- ... A portmanteau inhibitor is a drug that is a combination of two drug molecules, each of which is itself a type of inhibitor. The ...
KP-1461
It belongs to the class of nucleoside reverse transcriptase inhibitors.[citation needed] KP-1461 is a prodrug of the active ... Reverse transcriptase inhibitors, Experimental drugs, Prodrugs, All stub articles, Antiinfective agent stubs). ...
Katrin Rittinger
"Interface Peptides as Structure-based Human Immunodeficiency Virus Reverse Transcriptase Inhibitors". Journal of Biological ... Rittinger, K; Divita, G; Goody, R S (1995-08-15). "Human immunodeficiency virus reverse transcriptase substrate-induced ... Rittinger studied human immunodeficiency virus reverse transcriptase. At MRC National Institute for Medical Research Rittinger ... She has also collaborated with GlaxoSmithKline to discover inhibitors targeting the active site cysteine of thioester-forming ...
Didanosine
It is of the reverse-transcriptase inhibitor class. Didanosine was first described in 1975 and approved for use in the United ... Nucleoside analog reverse transcriptase inhibitors, Purines, Hepatotoxins, Bristol Myers Squibb, Hydroxymethyl compounds). ... Like other anti-HIV nucleoside analogs, it acts as a chain terminator by incorporation and inhibits viral reverse transcriptase ...
Emivirine
It is a non-nucleoside reverse transcriptase inhibitor. While emivirine showed promising antiviral activity in vitro, it failed ... Non-nucleoside reverse transcriptase inhibitors, Pyrimidinediones, Isopropyl compounds, Benzyl compounds, All stub articles, ...
Reverse transcription polymerase chain reaction
Then, add an RNase inhibitor and reverse transcriptase to the PCR tube. Next, place the PCR tube into a thermal cycler for one ... Once a one-step RT-PCR kit with a mix of reverse transcriptase, Taq DNA polymerase, and a proofreading polymerase is selected ... September 2002). "Development of a real-time reverse transcriptase PCR assay for type A influenza virus and the avian H5 and H7 ... The two-step reaction requires that the reverse transcriptase reaction and PCR amplification be performed in separate tubes. ...
Nucleoside triphosphate
Menéndez-Arias L (June 2008). "Mechanisms of resistance to nucleoside analogue inhibitors of HIV-1 reverse transcriptase". ...
Merle Sande
Trachtenberg, Joel D; Sande Merle A (July 2002). "Emerging resistance to nonnucleoside reverse transcriptase inhibitors: a ...
Entecavir
... is in the nucleoside reverse transcriptase inhibitors (NRTIs) family of medications. It prevents the hepatitis B ... Nucleoside analog reverse transcriptase inhibitors, Purines, Hepatotoxins, World Health Organization essential medicines, ... virus from multiplying by blocking reverse transcriptase. Entecavir was approved for medical use in 2005. It is on the World ... proven more selective potent inhibitor of HBV by virtue of being Guanine NA 1998: Inhibition of hepadnaviral polymerases was ...
Atevirdine
Ateviridine is a non-nucleoside reverse transcriptase inhibitor that has been studied for the treatment of HIV. Preparation of ... 1. A Novel Class of Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors". Journal of Medicinal Chemistry. 37 (7): 999-1014. ... Non-nucleoside reverse transcriptase inhibitors, Piperazines, Aminopyridines, All stub articles, Antiinfective agent stubs). ... amine with the imidazolide derivative of 5-methoxy-3-indoleacetic acid produces the amide reverse transcriptase inhibitor, ...
Amdoxovir
It acts as a nucleoside reverse transcriptase inhibitor (NRTI). The drug was discovered by Raymond F. Schinazi (Emory ... Nucleoside analog reverse transcriptase inhibitors, Purines, Dioxolanes, Experimental drugs, Hydroxymethyl compounds, All stub ...
Etravirine
... is a non-nucleoside reverse transcriptase inhibitor (NNRTI). Unlike the currently available agents in the class, ... Etravirine is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI), designed to be active against HIV ... who have evidence of viral replication and HIV-1 strains resistant to a non-nucleoside reverse transcriptase inhibitor (NNRTI) ... and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug- ...
Rovafovir etalafenamide
Nucleotide reverse transcriptase inhibitor, Treatment of HIV-1 infection". Drugs of the Future. 45 (7): 459. doi:10.1358/DOF. ... Rovafovir etalafenamide is a nucleotide reverse transcriptase inhibitor and prodrug of GS-9148. Rovafovir etalafenamide itself ... Reverse transcriptase inhibitors, Experimental drugs, Purines, Dihydrofurans, Ethyl esters, Phosphonate esters, All stub ... against viruses containing major mutations associated with resistance to the nucleoside analog reverse-transcriptase inhibitors ...
Rilpivirine
It is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with higher potency, longer half-life and ... Rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI). When taken by mouth, rilpivirine reaches highest ... Lade JM, Avery LB, Bumpus NN (October 2013). "Human biotransformation of the nonnucleoside reverse transcriptase inhibitor ... Non-nucleoside reverse transcriptase inhibitors, Nitriles, Pyrimidines, Johnson & Johnson brands). ...
Human T-lymphotropic virus
... a reverse-transcriptase inhibitor used for HIV; cepharanthine, an alkaloid from stephania cepharantha hayata; and phosphonated ... "Susceptibility of Primary HTLV-1 Isolates from Patients with HTLV-1-Associated Myelopathy to Reverse Transcriptase Inhibitors ... HTLV-1 infection is thought to spread only through dividing cells since reverse transcriptase generates proviral DNA from ...
Tenofovir disoproxil
... is a nucleotide analog reverse-transcriptase inhibitor (NtRTI). It selectively inhibits viral reverse ... It is a nucleotide reverse transcriptase inhibitor and works by decreasing the ability of the viruses to replicate. Tenofovir ... Nucleoside analog reverse transcriptase inhibitors, Prodrugs, Purines, World Health Organization essential medicines, Wikipedia ... the active compound that inhibits reverse transcriptase via chain termination. In fasting persons, bioavailability is 25%, and ...
Anisotropic Network Model
HIV-1 reverse transcriptase complexed with different inhibitors, by Temiz and Bahar, 2002. - HIV-1 protease, by Micheletti et ... application to alpha-amylase inhibitor", Doruker, P, Atilgan, AR & Bahar, I, Proteins, 15, 512-524, (2000). Hinsen, K. (1998) " ...
CYP3A4
Non-nucleoside reverse-transcriptase inhibitors have been shown to both induce and inhibit CYP3A4. Hidaka M, Fujita K, Ogikubo ... Inhibitors of CYP3A4 can be classified by their potency, such as: Strong inhibitor being one that causes at least a 5-fold ... Weak inhibitor being one that causes at least a 1.25-fold but less than 2-fold increase in the plasma AUC values, or 20-50% ... Moderate inhibitor being one that causes at least a 2-fold increase in the plasma AUC values, or 50-80% decrease in clearance. ...
Inte:Ligand
Other applications include the discovery of new Myeloperoxidase ligands, HIV reverse transcriptase inhibitors, applications in ... "Structure-Based Pharmacophore Identification of New Chemical Scaffolds as Non-Nucleoside Reverse Transcriptase Inhibitors". J. ... "Structure-Based Pharmacophore Identification of New Chemical Scaffolds as Non-Nucleoside Reverse Transcriptase Inhibitors". ... 3-dicarboxylic acid inhibitors of bacterial MurD and MurE ligases by structure-based virtual screening approach". Bioorganic & ...
Trifluoromethyl group
Some notable drugs containing trifluoromethyl groups include efavirenz (Sustiva), an HIV reverse transcriptase inhibitor; ...
List of DuPont Experimental Station inventions
Cozaar Losartan angiotensin II receptor antagonist to treat hypertension Sustiva Efavirenz reverse transcriptase inhibitor for ...
Index of biochemistry articles
Reverse transcriptase - RFLP - rho factor - rhodopsin - ribonucleoprotein - ribose - ribosomal protein - ribosomal protein S6 ... inhibitor - inhibitory gi G-protein - Inorganic chemistry - insect protein - Insulin - insulin receptor - insulin-like growth ...
Telomerase
TERT is a reverse transcriptase, which is a class of enzymes that creates single-stranded DNA using single-stranded RNA as a ... small-molecule and signal pathway inhibitors. The ability to maintain functional telomeres may be one mechanism that allows ... Telomerase is a reverse transcriptase enzyme that carries its own RNA molecule (e.g., with the sequence 3′-CCCAAUCCC-5′ in ... Vulliamy TJ, Walne A, Baskaradas A, Mason PJ, Marrone A, Dokal I (2005). "Mutations in the reverse transcriptase component of ...
Paul Lewi
In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodeficiency virus ...
Isatin
... and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors". Bioorg. Med. Chem. ... Mallamo, J.P. (2006). "Structure-guided identification of novel VEGFR-2 kinase inhibitors via solution phase parallel synthesis ... "Discovery of Tryptanthrin Derivatives as Potent Inhibitors of Indoleamine 2,3-Dioxygenase with Therapeutic Activity in Lewis ...
Telomerase RNA component
... with reverse transcriptase activity, and an RNA component, encoded by this gene, that serves as a template for the telomere ... Pruzan R, Pongracz K, Gietzen K, Wallweber G, Gryaznov S (January 2002). "Allosteric inhibitors of telomerase: oligonucleotide ... "Human telomerase activation requires two independent interactions between telomerase RNA and telomerase reverse transcriptase ... TERC serves as a template for telomere replication (reverse transcription) by telomerase. Telomerase RNAs differ greatly in ...
Microbicides for sexually transmitted diseases
... is a nucleotide reverse-transcriptase inhibitor (NRTI) which interferes with the replication of HIV and is approved in tablet ... a diarylpyrimidine inhibitor of HIV reverse transcriptase) and UC-781. These next-generation microbicides have received ...
Cabotegravir
... and when the virus has not developed resistance to non-nucleoside reverse transcriptase inhibitors (NNRTIs) and integrase ... It is an integrase inhibitor with a carbamoyl pyridone structure similar to that of dolutegravir. In December 2021, the U.S. ... Cabotegravir is an integrase strand transfer inhibitor. This means it blocks the HIV's enzyme integrase, thereby preventing its ... Integrase inhibitors, Fluoroarenes, Oxazolidines, 4-Pyridones, Heterocyclic compounds with 3 rings, Carboxamides). ...
Influenza
Most antiviral drugs against influenza fall into two categories: neuraminidase (NA) inhibitors and M2 inhibitors. Baloxavir ... Among NATs, reverse transcription polymerase chain reaction (RT-PCR) is the most traditional and considered the gold standard ... Three segments encode three subunits of an RNA-dependent RNA polymerase (RdRp) complex: PB1, a transcriptase, PB2, which ... NA inhibitors target the enzymatic activity of NA receptors, mimicking the binding of sialic acid in the active site of NA on ...
Foscarnet
Meyer PR, Rutvisuttinunt W, Matsuura SE, So AG, Scott WA (May 2007). "Stable complexes formed by HIV-1 reverse transcriptase at ... It is classified as a pyrophosphate analog DNA polymerase inhibitor. Foscarnet is the conjugate base of a chemical compound ... Meyer PR, Rutvisuttinunt W, Matsuura SE, So AG, Scott WA (2007). "Stable complexes formed by HIV-1 reverse transcriptase at ... In individuals treated with the DNA polymerase inhibitors acyclovir or ganciclovir, HSV or CMV particles can develop mutant ...
Division of Acquired Immunodeficiency Syndrome
... have shown that highly active antiretroviral therapy-regimens including reverse transcriptase and potent protease inhibitors- ... Moreover, damage to the immune system is incompletely reversed. Thus, there is an ongoing, urgent need for new therapeutic ...
Integrase
Mahboubi-Rabbani M, Abbasi M, Hajimahdi Z, Zarghi A (2021). "HIV-1 Reverse Transcriptase/Integrase Dual Inhibitors: A Review of ... The second integrase inhibitor, elvitegravir, was approved in the U.S. in August 2012. Integrase inhibitor Integron Beck BJ, ... Choi E, Mallareddy JR, Lu D, Kolluru S (October 2018). "Recent advances in the discovery of small-molecule inhibitors of HIV-1 ... production of the double-stranded linear viral DNA by the viral RNA/DNA-dependent DNA polymerase reverse transcriptase. The ...
María Blasco Marhuenda
"Telomerase reverse transcriptase delays aging in cancer resistant mice". Cell. 135 (4): 609-622. doi:10.1016/j.cell.2008.09.034 ... which are potent telomerase-inhibitors whose expression is altered in cancer; Demonstration that telomerase activity and ...
Elvucitabine
... of HIV drugs called nucleoside reverse transcriptase inhibitors (NRTIs). NRTIs block an HIV enzyme called reverse transcriptase ... Elvucitabine is an experimental nucleoside reverse transcriptase inhibitor (NRTI), developed by Achillion Pharmaceuticals, Inc ... Nucleoside analog reverse transcriptase inhibitors, Organofluorides, Pyrimidones, Experimental drugs, Hydroxymethyl compounds, ... An enzyme is a protein that starts or increases the speed of a chemical reaction). By blocking reverse transcriptase, NRTIs ...
Jean Nachega
He has shown that adherence to non-nucleoside reverse-transcriptase inhibitor HIV therapy has a linear dose-response pattern. ...
Cannabinoid
"Quantitative method to determine mRNA levels by reverse transcriptase-polymerase chain reaction from leukocyte subsets purified ... Thus supplementing with CYP 2C9 inhibitors leads to extended intoxication. Some is also stored in fat in addition to being ... Stout SM, Cimino NM (February 2014). "Exogenous cannabinoids as substrates, inhibitors, and inducers of human drug metabolizing ... cannabinoid-receptor ligands and inhibitors of anandamide inactivation with cannabimimetic activity in vitro and in vivo". The ...
Polymerase chain reaction
Reverse Transcription PCR (RT-PCR): for amplifying DNA from RNA. Reverse transcriptase reverse transcribes RNA into cDNA, which ... either by the binding of an antibody or by the presence of covalently bound inhibitors that dissociate only after a high- ... in this test the enzyme reverse transcriptase is used to generate a DNA sequence which matches the viral RNA; this DNA is then ... It is also sometimes abbreviated to RT-PCR (real-time PCR) but this abbreviation should be used only for reverse transcription ...
Clevudine
Nucleoside analog reverse transcriptase inhibitors, Pyrimidinediones, Organofluorides, Arabinosides, Halohydrins, Hydroxymethyl ...
Digital polymerase chain reaction
"Reverse transcriptase droplet digital PCR shows high resilience to PCR inhibitors from plant, soil and water samples". Plant ... dPCR is also more resilient to PCR inhibitors for the quantification of RNA than qPCR. dPCR can detect and quantify more ... been used to detect in a single well the expression of four different splice variants of human telomerase reverse transcriptase ... RNA quantification can be accomplished via RT-PCR, wherein RNA is reverse-transcribed into cDNA in the partitioned reaction ...
Hepatitis B virus
The nucleocapsid encloses the viral DNA and a DNA polymerase that has reverse transcriptase activity similar to retroviruses. ... Menéndez-Arias L, Álvarez M, Pacheco B (October 2014). "Nucleoside/nucleotide analog inhibitors of hepatitis B virus polymerase ... Hepatitis B is one of a few known non-retroviral viruses which use reverse transcription as a part of its replication process. ... long mRNA is then transported back to the cytoplasm where the virion P protein synthesizes DNA via its reverse transcriptase ...
Antiviral drug
... which uses reverse transcriptase as part of its replication process. Researchers have gone further and developed inhibitors ... Improved protease inhibitors are now in development. Protease inhibitors have also been seen in nature. A protease inhibitor ... This approach is more commonly associated with the inhibition of reverse transcriptase (RNA to DNA) than with "normal" ... An improved knowledge of the action of reverse transcriptase has led to better nucleoside analogues to treat HIV infections. ...
List of MeSH codes (D27)
... nucleic acid synthesis inhibitors MeSH D27.505.519.389.675.850 - reverse-transcriptase inhibitors MeSH D27.505.519.389.735 - ... hiv protease inhibitors MeSH D27.505.954.122.388.077.750 - reverse-transcriptase inhibitors MeSH D27.505.954.122.425 - ... enzyme inhibitors MeSH D27.505.519.389.099 - aromatase inhibitors MeSH D27.505.519.389.200 - carbonic anhydrase inhibitors MeSH ... trypsin inhibitors MeSH D27.505.519.389.755 - protein kinase inhibitors MeSH D27.505.519.389.760 - protein synthesis inhibitors ...
Thermus thermophilus
The enzyme possesses efficient reverse transcriptase activity in the presence of manganese. This enzyme is beneficial for ... it also has the capacity to detect RNA in the presence of inhibitors. Under the presence of inhibitors, it was shown to detect ... This polymerase has been shown to be resistant to DNA polymerase inhibitors present in clinical samples, ... "Capacity of rTth polymerase to detect RNA in the presence of various inhibitors". PLOS ONE. 13 (1): e0190041. Bibcode:2018PLoSO ...
Browsing by Subject "Reverse Transcriptase Inhibitors"
HIV Infection and AIDS Medication: Antiretroviral agent, nucleoside reverse-transcriptase inhibitor, Antiretroviral Agent,...
Three-drug combination of a non-nucleoside reverse transcriptase inhibitor, and two nucleo(t)side reverse transcriptase ... Combines integrase strand transfer inhibitor (INSTI) plus nucleoside reverse transcriptase inhibitor (NRTI). ... Antiretroviral agent, nucleoside reverse-transcriptase inhibitor. Class Summary. NRTIs agents inhibit viral replication by ... Antiretroviral agent, non-nucleoside reverse-transcriptase inhibitor. Class Summary. NNRTIs inhibit viral replication. ...
Nucleoside reverse transcriptase inhibitors (NRTIs or 'nukes') - HIV
FDA Accepts New Drug Applications for Merck's Doravirine, the Company's Investigational Non-Nucleoside Reverse Transcriptase...
Stereoselective Synthesis of Nucleoside Reverse Transcriptase Inhibitor (NRTI) BMS-986001
Cross-validated stepwise regression for identification of novel non-nucleoside reverse transcriptase inhibitor resistance...
This reduction in complexity was most significant for the non-nucleoside reverse transcriptase inhibitor (NNRTI) models, while ... Compared to standard stepwise regression we were able to reduce the number of mutations in the reverse transcriptase (RT) ... inhibitor models as well as the number of interaction terms accounting for synergistic and antagonistic effects. ... From: Cross-validated stepwise regression for identification of novel non-nucleoside reverse transcriptase inhibitor resistance ...
Level of viral load and antiretroviral resistance after 6 months of non-nucleoside reverse transcriptase inhibitor first-line...
Level of viral load and antiretroviral resistance after 6 months of non-nucleoside reverse transcriptase inhibitor first-line ... PATIENTS AND METHODS: Ninety-seven HIV-1-infected children who started two nucleoside reverse transcriptase inhibitors (NRTIs) ... and one non-nucleoside reverse transcriptase inhibitor (NNRTI) (mainly zidovudine/lamivudine/nevirapine) in Mali were ...
Natural presence of the V179D and K103R/V179D mutations associated with resistance to nonnucleoside reverse transcriptase...
... human immunodeficiency virus type 1 reverse transcriptase confer resistance to nonnucleoside reverse transcriptase inhibitors. ... Non-nucleoside reverse transcriptase inhibitor (NNRTI) cross-resistance: implications for preclinical evaluation of novel ... A uniquely prevalent nonnucleoside reverse transcriptase inhibitor resistance mutation in Russian subtype a HIV-1 viruses. AIDS ... Phenotypic susceptibility to nonnucleoside inhibitors of Virion-associated reverse transcriptase from different HIV types and ...
HEPT: From an investigation of lithiation of nucleosides towards a rational design of non-nucleoside reverse transcriptase...
CDC | TB | Managing Drug Interactions in the Treatment of HIV-Related Tuberculosis | Table 2a
HIV reverse transcriptase structures: designing new inhibitors and understanding mechanisms of drug resistance. - ORA - Oxford...
HIV reverse transcriptase (RT) is one of the main targets for the action of anti-AIDS drugs. The selection of drug-resistant ... "HIV Reverse Transcriptase Structures: Designing New Inhibitors and Understanding Mechanisms of Drug Resistance." Trends in ... "HIV Reverse Transcriptase Structures: Designing New Inhibitors and Understanding Mechanisms of Drug Resistance." Trends in ... HIV reverse transcriptase structures: designing new inhibitors and understanding mechanisms of drug resistance.. ...
Schedule Online - Nucleosides Reverse Transcriptase Inhibitors
"Nucleosides Reverse Transcriptase Inhibitors","data":{"category":"Medicine","linkRef":"Nucleosides Reverse Transcriptase ... "Non-nucleosides Reverse Transcriptase Inhibitors","data":{"category":"Medicine","linkRef":"Non-nucleosides Reverse ... ":"ACE Inhibitors"}},{"value":"ACE Inhibitors with Diuretics","data":{"category":"Medicine","linkRef":"ACE Inhibitors with ... Transcriptase Inhibitors"}},{"value":"Non-opioid Analgesics","data":{"category":"Medicine","linkRef":"Non-opioid Analgesics ...
Potent nonnucleoside reverse transcriptase inhibitors target HIV-1 Gag-Pol. | Burnet Institute
Nonnucleoside reverse transcriptase inhibitors (NNRTIs) target HIV-1 reverse transcriptase (RT) by binding to a pocket in RT ... HIV reverse transcriptase structure function and role in HIV replication. To study the role of reverse transcriptase ... Potent nonnucleoside reverse transcriptase inhibitors target HIV-1 Gag-Pol.. Figueiredo A, Moore KL, Mak J, Sluis-Cremer N, de ... NNRTIs, in particular, those that are potent inhibitors of RT polymerase activity, can also act as chemical enhancers of the ...
CYP
Synthesis, bioactivity, 3D-QSAR studies of novel HIV-1 reverse transcriptase inhibitors ... Synthesis, bioactivity, 3D-QSAR studies of novel HIV-1 reverse transcriptase inhibitors ... HIV-1 reverse transcriptase inhibitor Category: CYP. Another important concern is that CSF examples cannot be extracted from a ...
DNA Ligases
Pharmacokinetic, pharmacodynamic and clinical profile of HIV-1 Reverse Transcriptase inhibitors. HIV-1 Reverse Transcriptase ... Pharmacokinetic, pharmacodynamic and clinical profile of HIV-1 Reverse Transcriptase inhibitors © 2022. All Rights Reserved. ... of proinflammatory cytokines restored acute morphine antinociception in nerve-injured rats and also significantly reversed the ...
Low rates of nucleoside reverse transcriptase inhibitor and nonnucleoside reverse transcriptase inhibitor drug resistance in...
Low rates of nucleoside reverse transcriptase inhibitor and nonnucleoside reverse transcriptase inhibitor drug resistance in ... Low rates of nucleoside reverse transcriptase inhibitor and nonnucleoside reverse transcriptase inhibitor drug resistance in ... Title : Low rates of nucleoside reverse transcriptase inhibitor and nonnucleoside reverse transcriptase inhibitor drug ... associated with nucleoside reverse transcriptase inhibitors (NRTI) and nonnucleoside reverse transcriptase inhibitors (NNRTI) ...
HIV/AIDS Medications - POZ
Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs) Learn more ,, More ,, DRUG ABBRV. GENERIC NAME. ... Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) Learn more ,, More ,, DRUG ABBRV. GENERIC NAME. ... Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs) * Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) ...
Table 1 - Inhibition of SARS Coronavirus Infection In Vitro with Clinically Approved Antiviral Drugs - Volume 10, Number 4...
Scholar Commons @ Tower Health - Tower Health Research Day: Nucleoside Reverse Transcriptase Inhibitors Induced Lactic Acidosis
Browsing by Subject
Tenofovir
IMSEAR at SEARO: High performance liquid chromatographic assay for the determination of Protease Inhibitors (PIs) and Non...
... and Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs) in human plasma. Siriraj Medical Journal, 2012 Jan; 64(1): 1-6. ... and Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs) in human plasma.. 作者: Sangsiriwut, Kantima. Anekthananon, ... and two non-nucleoside reverse transcriptase inhibitors (NNRTIs): nevirapine (NVP), and efavirenz (EFV) in human plasma. ... The compounds were separated on a reversed-phase C18 column with gradient phase of 25 mM phosphate buffer (pH 4.9) and ...
Pediatric HIV Infection Medication: Nucleoside or Nucleotide Reverse Transcriptase Inhibitors, Nonnucleoside Reverse...
Three-drug combination of a non-nucleoside reverse transcriptase inhibitor, and two nucleo(t)side reverse transcriptase ... Nucleoside or Nucleotide Reverse Transcriptase Inhibitors. Class Summary. NRTIs are nucleoside or nucleotide reverse ... CYP3A inhibitor), and emtricitabine and tenofovir alafenamide (TAF), both nucleoside analog reverse transcriptase inhibitors ( ... Nonnucleoside Reverse Transcriptase Inhibitors. Class Summary. NNRTIs inhibit both DNA-directed and RNA-directed polymerase ...
Analysis of nonnucleoside drug-resistant variants of human immunodeficiency virus type 1 reverse transcriptase
... reverse transcriptase (RT) have been reported. Several lines of evidence, including the isolation of RT mutants that show cross ... A number of chemically distinct nonnucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) ... A number of chemically distinct nonnucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase ( ... Analysis of nonnucleoside drug-resistant variants of human immunodeficiency virus type 1 reverse transcriptase J Virol. 1993 ...
Update to U.S. Medical Eligibility Criteria for Contraceptive Use, 2016: Updated Recommendations for the Use of Contraception...
Polbase - Reference: Biochemical and mechanistic basis for the activity of nucleoside analogue inhibitors of HIV reverse...
Biochemical and mechanistic basis for the activity of nucleoside analogue inhibitors of HIV reverse transcriptase. ... the nucleoside reverse transcriptase inhibitors (NRTIs) and the non-nucleoside reverse transcriptase inhibitors (NNRTIs), act ... Biochemical and mechanistic basis for the activity of nucleoside analogue inhibitors of HIV reverse transcriptase. Reverse ... reverse transcriptase, RT) ... HIV encodes an RNA directed DNA polymerase (reverse transcriptase, RT) that is an essential ...
LINE1 Reverse Transcriptase Inhibitors Abrogate Type 1 Interferon Responses | American College of Rheumatology Convergence 2022...
Replicative fitness costs of nonnucleoside reverse transcriptase inhibitor drug resistance mutations on HIV subtype C. |...
This study investigates how nonnucleoside reverse transcriptase inhibitor (NNRTI) drug resistance mutations of subtype C affect ... Replicative fitness costs of nonnucleoside reverse transcriptase inhibitor drug resistance mutations on HIV subtype C.. ... The 103N, 106A, 106M, 181C, 188C, 188L, and 190A drug resistance mutations were placed in a reverse transcriptase (RT) that ... HIV/efeitos dos fármacos HIV/genética Inibidores da Transcriptase Reversa/farmacologia Linhagem Celular Farmacorresistência ...
Horsetail: MedlinePlus Supplements
NRTIsNNRTINNRTIsProtease inhibitorNRTINonnucleoside reverse transcripPolymerase Chain ReAntiretroviral therapyMutationsResistanceRegimensInhibitsNucleotide analogInhibitory activityEnzymeSelectiveAssayPotentFusionDrugInactivationSubstrates2021TranscriptionToxicityDoseRifampinActivityTreatmentAdultsReplicationDrugs
NRTIs7
- Ninety-seven HIV-1-infected children who started two nucleoside reverse transcriptase inhibitors (NRTIs) and one non-nucleoside reverse transcriptase inhibitor (NNRTI) (mainly zidovudine/lamivudine/nevirapine) in Mali were prospectively studied. (pasteur.fr)
- Initial therapy should be started with a combination of 3 ARTs, including a backbone of 2 NRTIs plus an NNRTI, or 2 NRTIs plus a protease inhibitor. (medscape.com)
- NRTIs are nucleoside or nucleotide reverse transcriptase inhibitor analogs with antiretroviral activity. (medscape.com)
- Two of the four classes of currently approved anti-HIV drugs, the nucleoside reverse transcriptase inhibitors (NRTIs) and the non-nucleoside reverse transcriptase inhibitors (NNRTIs), act by inhibiting this enzyme. (neb.com)
- PZA PZA include protease inhibitors, NRTIs, and NNRTIs. (cdc.gov)
- Methods: In a randomised open-label factorial trial, we compared effectiveness of two nucleoside reverse transcriptase inhibitors (NRTIs) plus a protease inhibitor versus two NRTIs plus an NNRTI and of switch to second-line ART at a viral load of 1000 copies per mL versus 30 000 copies per mL in previously untreated children infected with HIV from Europe and North and South America. (elsevier.com)
- NRTIs and integrase inhibitors interfere with the action of the two enzymes to prevent the virus from replicating and further infecting cells. (gsk.com)
NNRTI5
- This study investigates how nonnucleoside reverse transcriptase inhibitor (NNRTI) drug resistance mutations of subtype C affect replication capacity. (bvsalud.org)
- nonnucleaoside reverse transcriptase inhibitors (NNRTI), protease inhibitors (PI), fusion inhibitors, integrase trans transfer inhibitors (INSTI), and CCR5 Antagonists. (homeworkshine.com)
- The different classes of drug regimens include: nucleoside reverse transcriptase inhibitors (NRTI), nonnucleaoside reverse transcriptase inhibitors (NNRTI), protease inhibitors (PI), fusion inhibitors, integrase trans transfer inhibitors (INSTI), and CCR5 Antagonists. (homeworkshine.com)
- We assess the long-term outcome of protease inhibitor and non-nucleoside reverse transcriptase inhibitor (NNRTI) first-line ART and viral load switch criteria in children. (elsevier.com)
- IQR 2·8-12·9) were randomly assigned treatment regimens: 66 to receive protease inhibitor and switch to second-line at 1000 copies per mL (PI-low), 65 protease inhibitor and switch at 30 000 copies per mL (PI-higher), 68 NNRTI and switch at 1000 copies per mL (NNRTI-low), and 67 NNRTI and switch at 30 000 copies per mL (NNRTI-higher). (elsevier.com)
NNRTIs12
- For example, most of the HIV-1 O group viruses are considered to be naturally resistant to nonnucleoside reverse transcriptase inhibitors (NNRTIs) due to the presence of the Y181C mutation [ 7 ]. (biomedcentral.com)
- All non-nucleoside reverse transcriptase inhibitors (NNRTIs) are metabolized in the liver by CYP3A isoenzymes. (medscape.com)
- Nonnucleoside reverse transcriptase inhibitors (NNRTIs) target HIV-1 reverse transcriptase (RT) by binding to a pocket in RT that is close to, but distinct, from the DNA polymerase active site and prevent the synthesis of viral cDNA. (edu.au)
- NNRTIs, in particular, those that are potent inhibitors of RT polymerase activity, can also act as chemical enhancers of the enzyme's inter-subunit interactions. (edu.au)
- IMSEAR at SEARO: High performance liquid chromatographic assay for the determination of Protease Inhibitors (PIs) and Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs) in human plasma. (who.int)
- Objective: To develop and validate a high performance liquid chromatography (HPLC) method for simultaneous quantitative determination of five HIV protease inhibitors (PIs): indinavir (IDV), lopinavir (LPV), nelfinavir (NFV), ritonavir (RTV), saquinavir (SQV), and two non-nucleoside reverse transcriptase inhibitors (NNRTIs): nevirapine (NVP), and efavirenz (EFV) in human plasma. (who.int)
- or or A 20%-25% increase in the dose of protease inhibitors or NNRTIs might be necessary. (cdc.gov)
- INH Daily for 2 weeks and INH 2 times/week for The patient should be monitored If the patient also is taking RFB then 2 times/week for RFB 4 months (18 weeks) carefully for RFB drug toxicity efavirenz, the daily or twice (arthalgia, uveitis,leukopenia) weekly dose of RFB is increased if RFB is used concurrently from 300mg to 450 mg. with protease inhibitors or NNRTIs. (cdc.gov)
- Six-month RIF-based therapy (may be prolonged* to 9 months) ------------------------------------------------------------------------------------------------------------------------------------------------------------------- A.I INH Daily for 2 months INH Daily or 2-3 times/week Protease inhibitors or NNRTIs SM is contraindicated for RIF (8 weeks) RIF for 4 months (18 weeks) should not be administered pregnant women. (cdc.gov)
- However, the rapid emergence of drug-resistant strains and unsatisfactory drug-like properties seriously limit the clinical application of HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs). (bvsalud.org)
- The target inhibitor ZA-2 with a fluorosulfate warhead in the structure was found to be a potent inhibitor (EC50 = 11-246 nM) against HIV-1 IIIB and a panel of NNRTIs-resistant strains, being far superior to those of NVP and EFV. (bvsalud.org)
- Although non-nucleoside reverse transcriptase inhibitors (NNRTIs) exhibit potent anti-HIV-1 activity and play an important role in the active antiretroviral therapy of AIDS, the emergence of drug-resistant strains has seriously reduced their clinical efficacy. (bvsalud.org)
Protease inhibitor2
- Protease inhibitor resistance was uncommon and there was no increase in NRTI resistance in the PI-higher compared with the PI-low group. (elsevier.com)
- Delayed switching of protease-inhibitor-based ART might be reasonable where future drug options are limited, because the risk of selecting for NRTI and protease-inhibitor resistance is low. (elsevier.com)
NRTI1
- A nucleoside analogue reverse transcriptase inhibitor (NRTI) with antiretroviral activity against HIV, it is used (particularly as the sulfate) with other antiretrovirals in combination therapy of HIV infection. (ebi.ac.uk)
Nonnucleoside reverse transcrip1
- Replicative fitness costs of nonnucleoside reverse transcriptase inhibitor drug resistance mutations on HIV subtype C. (bvsalud.org)
Polymerase Chain Re1
- Standard reverse transcription-polymerase chain reaction (RT-PCR) can be done with INCB018424 biological activity smaller amounts of RNA (20C40 ng), but quantification is hard and relies on endpoint analysis of the PCR product. (irjs.info)
Antiretroviral therapy1
- 1. Rinkman K, Smeitink JA, Romijn JA, Reiss P. Mitochondrial toxicity induced by nucleoside-analogue reverse-transcriptase inhibitors is a key factor in the pathogenesis of antiretroviral-therapy-related lipodystrophy. (bvsalud.org)
Mutations1
- The 103N, 106A, 106M, 181C, 188C, 188L, and 190A drug resistance mutations were placed in a reverse transcriptase (RT) that matches the consensus subtype C sequence as well as the HXB2 RT, as a subtype B reference. (bvsalud.org)
Resistance6
- HIV reverse transcriptase structures: designing new inhibitors and understanding mechanisms of drug resistance. (ox.ac.uk)
- Several lines of evidence, including the isolation of RT mutants that show cross resistance, suggest that, despite their structural diversity, many of these inhibitors bind to a common site on HIV-1 RT. (nih.gov)
- We have used BspMI cassette mutagenesis to prepare a collection of HIV-1 RT mutants that show resistance to the known members of the general class of nonnucleoside inhibitors. (nih.gov)
- This collection of mutants can be used to determine whether a new drug will show cross resistance with known inhibitors and to define amino acid positions critical for the action of the drugs. (nih.gov)
- This study presents proof of concept for designing a novel HIV-1 covalent inhibitor targeting the highly conserved Tyr318 in the HIV-1 non-nucleoside reverse transcriptase inhibitors binding pocket to improve the drug resistance profiles. (bvsalud.org)
- Carbovir Triphosphate Triethylamine Salt (Abacavir - In House Impurity) is an active metabolite of Abacavir (A104990) used to study the molecular mechanism of inhibition and drug resistance for HIV-1 reverse transcriptase (1, 2, 3). (hoelzel-biotech.com)
Regimens1
- The mean time on ART was 75.5 months (95% confidence interval [CI]: 69.0-81.9 months), and 93.7% of the patients were receiving non-nucleoside reverse transcriptase inhibitor-based regimens. (who.int)
Inhibits5
- It inhibits activity of HIV reverse transcriptase by competing with natural substrate for use by and incorporation into viral DNA. (medscape.com)
- This antiretroviral agent used in treatment of AIDS inhibits activity of HIV reverse transcriptase by competing with natural substrate deoxyadenosine 5'-triphosphate and, after incorporation into DNA, by causing DNA chain termination. (medscape.com)
- An entity which inhibits the activity of HIV-1 reverse transcriptase. (ebi.ac.uk)
- RNase H inhibitors have been explored as an anti-HIV drug target because RNase H inactivation inhibits reverse transcription. (unl.edu)
- mTOR kinase inhibitor AZD2014 inhibits the activity of mTOR, which may result in the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. (biochempartner.com)
Nucleotide analog2
- Sovaldi belongs to a group of drugs called nucleotide analog polymerase inhibitors. (rxwiki.com)
- Based on drug class, the global hepatitis therapeutics market has been categorized into nucleotide analog reverse transcriptase inhibitor, NS5A inhibitor, multi- class combination, nucleotide analog NS5B polymerase inhibitor, interferon & ribavirin, and others. (clickpress.com)
Inhibitory activity2
- Wang, H. X. and Ng, T. B. Examination of lectins, polysaccharopeptide, polysaccharide, alkaloid, coumarin and trypsin inhibitors for inhibitory activity against human immunodeficiency virus reverse transcriptase and glycohydrolases. (webmd.com)
- The co-crystal structure analysis and molecular dynamics simulation studies were conducted to explain the broad-spectrum inhibitory activity of 18b1 against reverse transcriptase variants. (bvsalud.org)
Enzyme5
- It does this by using an enzyme called reverse transcriptase. (va.gov)
- HIV encodes an RNA directed DNA polymerase (reverse transcriptase, RT) that is an essential enzyme in the viral replication cycle. (neb.com)
- Inhibitors of reverse transcriptase (RNA-DIRECTED DNA POLYMERASE), an enzyme that synthesizes DNA on an RNA template. (bvsalud.org)
- In the reverse transcriptase inhibitory assay, ZA-2 exhibited an IC50 value of 0.057 µM with the ELISA method, and the MALDI-TOF MS data demonstrated the covalent binding mode of ZA-2 with the enzyme. (bvsalud.org)
- 1, 2, 3 The performance of the reverse transcription (RT) response may be suffering from the enzyme, primers, nucleotides, and RNA secondary framework. (irjs.info)
Selective1
- In order to identify highly selective and potent BuChE inhibitors, a 53-membered compound library was constructed via the oxime-based tethering approach based on microscale synthesis. (bvsalud.org)
Assay1
- be detected using real-time quantitative reverse transcriptase-PCR, and this assay revealed a statistical link between hTERT mRNA levels and the aggressiveness of breast tumors [12]. (asiatox.org)
Potent1
- Potent nonnucleoside reverse transcriptase inhibitors target HIV-1 Gag-Pol. (edu.au)
Fusion1
- Fusion inhibitors prevents HIV from entering the cells by blocking the fusion process of the virus to the membrane of the CD4 T cells. (homeworkshine.com)
Drug1
- This guideline presents updated data about drug interactions between protease inhibitors and non-nucleoside reverse transcriptase inhibitors for treatment of HIV infection together with rifamycins for treatment of TB. (cdc.gov)
Inactivation1
- Amplification for RT was done as follows: initial incubation step at 25 ºC for 10 min, followed by a reverse transcription step at 48 ºC for 30 min and a reverse transcriptase inactivation step at 95 ºC for 5 min in a GeneAmp® PCR system 9700 (Applied Biosystems, USA). (docsbay.net)
Substrates1
- Encorafenib (a BCRP inhibitor) may increase the concentration and toxicities of BCRP substrates. (medscape.com)
20211
- Gupta, Riju, "Nucleoside Reverse Transcriptase Inhibitors Induced Lactic Acidosis" (2021). (towerhealth.org)
Transcription2
- The reverse transcription (RT) reaction mixture contained 2.5 µg of total RNA, 1X TaqMan RT buffer, 5.5 mM magnesium chloride, 500 µM of each dNTP, 2.5 µM olig-dT, 0.4 U µL-1 RNase inhibitor, and 1.25 U µL-1 MultiScribe reverse transcriptase in a total reaction volume of 100 µL. (docsbay.net)
- DNA polymerases, PCR Master Mixes, qPCR Mixes and reverse transcription reagents are highly valued across the globe. (solisbiodyne.com)
Toxicity1
- Treatment with telomerase inhibitors may not have the toxicity found with other chemotherapeutic brokers since telomerase is usually absent in most somatic cells (Fig. (asiatox.org)
Dose1
- The twice-weekly dose of RFB (300mg) remains unchanged if the patient is also taking these protease inhibitors. (cdc.gov)
Rifampin1
- Guidelines for the Use of Rifabutin or Rifampin for the Treatment and Prevention of Tuberculosis among HIV-Infected Patients Taking Protease Inhibitors or Non-Nucleoside Reverse Transcriptase Inhibitors. (cdc.gov)
Activity2
- Reference: Biochemical and mechanistic basis for the activity of nucleoside analogue inhibitors of HIV reverse transcriptase. (neb.com)
- Vistusertib, also known as AZD2014, is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity. (biochempartner.com)
Treatment2
- HIV-1 reverse transcriptase is one of the most attractive targets for the treatment of AIDS. (bvsalud.org)
- Since most breast cancer cells have very short telomeres, treatment with telomerase inhibitors should lead to growth arrest and cell death. (asiatox.org)
Adults1
- 971 adults on Non-Nucleoside Reverse Transcriptase Inhibitors were included. (academicjournals.org)
Replication3
- To study the role of reverse transcriptase dimerization in HIV replication. (edu.au)
- Protease inhibitors target the cell replication in the later stages. (homeworkshine.com)
- Further, circularized viral DNA, a marker of recent nuclear import of full-length, reverse-transcribed RNA, has been detected in kidney biopsy samples from patients with HIVAN, suggesting active replication in renal tissue. (medscape.com)