Inhibitors of reverse transcriptase (RNA-DIRECTED DNA POLYMERASE), an enzyme that synthesizes DNA on an RNA template.
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.
Agents used to treat AIDS and/or stop the spread of the HIV infection. These do not include drugs used to treat symptoms or opportunistic infections associated with AIDS.
The ability of viruses to resist or to become tolerant to chemotherapeutic agents or antiviral agents. This resistance is acquired through gene mutation.
The type species of LENTIVIRUS and the etiologic agent of AIDS. It is characterized by its cytopathic effect and affinity for the T4-lymphocyte.
OXAZINES with a fused BENZENE ring.
A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS.
Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).
A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group.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.
A potent, non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1.
Inhibitors of HIV PROTEASE, an enzyme required for production of proteins needed for viral assembly.
An enzyme that synthesizes DNA on an RNA template. It is encoded by the pol gene of retroviruses and by certain retrovirus-like elements. EC 2.7.7.49.
Carbon-containing phosphonic acid compounds. Included under this heading are compounds that have carbon bound to either OXYGEN atom or the PHOSPHOROUS atom of the (P=O)O2 structure.
A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.
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.
The ability of viruses to resist or to become tolerant to several structurally and functionally distinct drugs simultaneously. This resistance phenotype may be attributed to multiple gene mutation.
A purine base and a fundamental unit of ADENINE NUCLEOTIDES.
Six-membered heterocycles containing an oxygen and a nitrogen.
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.
Drug regimens, for patients with HIV INFECTIONS, that aggressively suppress HIV replication. The regimens usually involve administration of three or more different drugs including a protease inhibitor.
A reverse transcriptase inhibitor and ZALCITABINE analog in which a sulfur atom replaces the 3' carbon of the pentose ring. It is used to treat HIV disease.
A type of COUMARINS with added pyran ring(s).
Purine or pyrimidine bases attached to a ribose or deoxyribose. (From King & Stansfield, A Dictionary of Genetics, 4th ed)
An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.
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.
An HIV protease inhibitor used in a fixed-dose combination with RITONAVIR. It is also an inhibitor of CYTOCHROME P-450 CYP3A.
The phosphate esters of DIDEOXYNUCLEOSIDES.
The quantity of measurable virus in a body fluid. Change in viral load, measured in plasma, is sometimes used as a SURROGATE MARKER in disease progression.
Agents used to treat RETROVIRIDAE INFECTIONS.
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.
The number of CD4-POSITIVE T-LYMPHOCYTES per unit volume of BLOOD. Determination requires the use of a fluorescence-activated flow cytometer.
Therapy with two or more separate preparations given for a combined effect.
Ribonucleic acid that makes up the genetic material of viruses.
Any detectable and heritable change in the genetic material that causes a change in the GENOTYPE and which is transmitted to daughter cells and to succeeding generations.
A measure of the quality of health care by assessment of unsuccessful results of management and procedures used in combating disease, in individual cases or series.
The process of intracellular viral multiplication, consisting of the synthesis of PROTEINS; NUCLEIC ACIDS; and sometimes LIPIDS, and their assembly into a new infectious particle.
Enzyme of the human immunodeficiency virus that is required for post-translational cleavage of gag and gag-pol precursor polyproteins into functional products needed for viral assembly. HIV protease is an aspartic protease encoded by the amino terminus of the pol gene.
A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.
A ribonuclease that specifically cleaves the RNA moiety of RNA:DNA hybrids. It has been isolated from a wide variety of prokaryotic and eukaryotic organisms as well as RETROVIRUSES.
Inhibitors of HIV INTEGRASE, an enzyme required for integration of viral DNA into cellular DNA.
Defective metabolism leading to fat maldistribution in patients infected with HIV. The etiology appears to be multifactorial and probably involves some combination of infection-induced alterations in metabolism, direct effects of antiretroviral therapy, and patient-related factors.
An essential ribonucleoprotein reverse transcriptase that adds telomeric DNA to the ends of eukaryotic CHROMOSOMES.
A variation of the PCR technique in which cDNA is made from RNA via reverse transcription. The resultant cDNA is then amplified using standard PCR protocols.
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.
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
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.
Phosphate esters of THYMIDINE in N-glycosidic linkage with ribose or deoxyribose, as occurs in nucleic acids. (From Dorland, 28th ed, p1154)
Acidosis caused by accumulation of lactic acid more rapidly than it can be metabolized. It may occur spontaneously or in association with diseases such as DIABETES MELLITUS; LEUKEMIA; or LIVER FAILURE.
The biosynthesis of DNA carried out on a template of RNA.
Proteins encoded by the POL GENE of the HUMAN IMMUNODEFICIENCY VIRUS.
A mutation in which a codon is mutated to one directing the incorporation of a different amino acid. This substitution may result in an inactive or unstable product. (From A Dictionary of Genetics, King & Stansfield, 5th ed)
Compounds which inhibit or antagonize biosynthesis or actions of integrase.
The genetic constitution of the individual, comprising the ALLELES present at each GENETIC LOCUS.
Compounds with a 5-membered ring of four carbons and an oxygen. They are aromatic heterocycles. The reduced form is tetrahydrofuran.
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.
An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases, and also inhibits CYTOCHROME P-450 CYP3A.
A potent and specific HIV protease inhibitor that appears to have good oral bioavailability.
A group of compounds that are derivatives of oxo-pyrrolidines. A member of this group is 2-oxo pyrrolidine, which is an intermediate in the manufacture of polyvinylpyrrolidone. (From Merck Index, 11th ed)
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.
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
Organic compounds containing the -CN radical. The concept is distinguished from CYANIDES, which denotes inorganic salts of HYDROGEN CYANIDE.
The ability of microorganisms, especially bacteria, to resist or to become tolerant to chemotherapeutic agents, antimicrobial agents, or antibiotics. This resistance may be acquired through gene mutation or foreign DNA in transmissible plasmids (R FACTORS).
Established cell cultures that have the potential to propagate indefinitely.
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.
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
The concentration of a compound needed to reduce population growth of organisms, including eukaryotic cells, by 50% in vitro. Though often expressed to denote in vitro antibacterial activity, it is also used as a benchmark for cytotoxicity to eukaryotic cells in culture.
Compounds which inhibit or antagonize biosynthesis or actions of proteases (ENDOPEPTIDASES).
Pyridine derivatives with one or more keto groups on the ring.
A species of ALPHARETROVIRUS causing anemia in fowl.
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.
An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV.
Deoxyribonucleic acid that makes up the genetic material of viruses.
A species of the genus ERYTHROCEBUS, subfamily CERCOPITHECINAE, family CERCOPITHECIDAE. It inhabits the flat open arid country of Africa. It is also known as the patas monkey or the red monkey.
Double-stranded DNA of MITOCHONDRIA. In eukaryotes, the mitochondrial GENOME is circular and codes for ribosomal RNAs, transfer RNAs, and about 10 proteins.
Inorganic or organic compounds that contain sulfur as an integral part of the molecule.
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)
Macromolecular molds for the synthesis of complementary macromolecules, as in DNA REPLICATION; GENETIC TRANSCRIPTION of DNA to RNA, and GENETIC TRANSLATION of RNA into POLYPEPTIDES.
Any tests that demonstrate the relative efficacy of different chemotherapeutic agents against specific microorganisms (i.e., bacteria, fungi, viruses).
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.
Evaluation undertaken to assess the results or consequences of management and procedures used in combating disease in order to determine the efficacy, effectiveness, safety, and practicability of these interventions in individual cases or series.
A family of 6-membered heterocyclic compounds occurring in nature in a wide variety of forms. They include several nucleic acid constituents (CYTOSINE; THYMINE; and URACIL) and form the basic structure of the barbiturates.
Mature LYMPHOCYTES and MONOCYTES transported by the blood to the body's extravascular space. They are morphologically distinguishable from mature granulocytic leukocytes by their large, non-lobed nuclei and lack of coarse, heavily stained cytoplasmic granules.
Adenosine molecules which can be substituted in any position, but are lacking one hydroxyl group in the ribose part of the molecule.
A republic in southern Africa, between NAMIBIA and ZAMBIA. It was formerly called Bechuanaland. Its capital is Gaborone. The Kalahari Desert is in the west and southwest.
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
Short sequences (generally about 10 base pairs) of DNA that are complementary to sequences of messenger RNA and allow reverse transcriptases to start copying the adjacent sequences of mRNA. Primers are used extensively in genetic and molecular biology techniques.
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
A multistage process that includes cloning, physical mapping, subcloning, determination of the DNA SEQUENCE, and information analysis.
Single preparations containing two or more active agents, for the purpose of their concurrent administration as a fixed dose mixture.
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.
Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.
The rate dynamics in chemical or physical systems.
Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.
The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
Inhibitors of the fusion of HIV to host cells, preventing viral entry. This includes compounds that block attachment of HIV ENVELOPE PROTEIN GP120 to CD4 RECEPTORS.
Elements of limited time intervals, contributing to particular results or situations.
The relationship between the dose of an administered drug and the response of the organism to the drug.
Time schedule for administration of a drug in order to achieve optimum effectiveness and convenience.
Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications.
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.
Genetically engineered MUTAGENESIS at a specific site in the DNA molecule that introduces a base substitution, or an insertion or deletion.
A group of compounds that contain the structure SO2NH2.
Keto-pyrans.
The transmission of infectious disease or pathogens from one generation to another. It includes transmission in utero or intrapartum by exposure to blood and secretions, and postpartum exposure via breastfeeding.
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.
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)
The residual portion of BLOOD that is left after removal of BLOOD CELLS by CENTRIFUGATION without prior BLOOD COAGULATION.
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.
The outward appearance of the individual. It is the product of interactions between genes, and between the GENOTYPE and the environment.
Species of the genus LENTIVIRUS, subgenus primate immunodeficiency viruses (IMMUNODEFICIENCY VIRUSES, PRIMATE), that induces acquired immunodeficiency syndrome in monkeys and apes (SAIDS). The genetic organization of SIV is virtually identical to HIV.
Organic compounds that contain phosphorus as an integral part of the molecule. Included under this heading is broad array of synthetic compounds that are used as PESTICIDES and DRUGS.
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.
Voluntary cooperation of the patient in following a prescribed regimen.
The relationships of groups of organisms as reflected by their genetic makeup.
Colloids with a solid continuous phase and liquid as the dispersed phase; gels may be unstable when, due to temperature or other cause, the solid phase liquefies; the resulting colloid is called a sol.
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.
The insertion of drugs into the vagina to treat local infections, neoplasms, or to induce labor. The dosage forms may include medicated pessaries, irrigation fluids, and suppositories.
The co-occurrence of pregnancy and an INFECTION. The infection may precede or follow FERTILIZATION.
Six-carbon alicyclic hydrocarbons.
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.
The action of a drug in promoting or enhancing the effectiveness of another drug.
The process of observing, recording, or detecting the effects of a chemical substance administered to an individual therapeutically or diagnostically.
The presence of viruses in the blood.
The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
Proteins prepared by recombinant DNA technology.
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.
Development of neutralizing antibodies in individuals who have been exposed to the human immunodeficiency virus (HIV/HTLV-III/LAV).
A transfer RNA which is specific for carrying lysine to sites on the ribosomes in preparation for protein synthesis.
A strain of Murine leukemia virus (LEUKEMIA VIRUS, MURINE) arising during the propagation of S37 mouse sarcoma, and causing lymphoid leukemia in mice. It also infects rats and newborn hamsters. It is apparently transmitted to embryos in utero and to newborns through mother's milk.
Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.
DNA sequences that form the coding region for retroviral enzymes including reverse transcriptase, protease, and endonuclease/integrase. "pol" is short for polymerase, the enzyme class of reverse transcriptase.
Determination of the spectra of ultraviolet absorption by specific molecules in gases or liquids, for example Cl2, SO2, NO2, CS2, ozone, mercury vapor, and various unsaturated compounds. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
Simultaneous resistance to several structurally and functionally distinct drugs.
A species of the genus MACACA inhabiting India, China, and other parts of Asia. The species is used extensively in biomedical research and adapts very well to living with humans.
Acquired defect of cellular immunity that occurs naturally in macaques infected with SRV serotypes, experimentally in monkeys inoculated with SRV or MASON-PFIZER MONKEY VIRUS; (MPMV), or in monkeys infected with SIMIAN IMMUNODEFICIENCY VIRUS.
A republic in southern Africa, the southernmost part of Africa. It has three capitals: Pretoria (administrative), Cape Town (legislative), and Bloemfontein (judicial). Officially the Republic of South Africa since 1960, it was called the Union of South Africa 1910-1960.
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)
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.
The total number of cases of a given disease in a specified population at a designated time. It is differentiated from INCIDENCE, which refers to the number of new cases in the population at a given time.
Observation of a population for a sufficient number of persons over a sufficient number of years to generate incidence or mortality rates subsequent to the selection of the study group.
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.
The type species of ALPHARETROVIRUS producing latent or manifest lymphoid leukosis in fowl.
Guanine nucleotides which contain deoxyribose as the sugar moiety.
The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action.

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)

Information on antiretroviral dosing errors among health care providers for outpatient human immunodeficiency virus (HIV)-infected patients is lacking. We evaluated factors associated with nucleoside reverse-transcriptase inhibitor dosing errors in a university-based HIV clinic using an electronic medical record. Overall, older age, minority race or ethnicity, and didanosine use were related to such errors. Impaired renal function was more common in older patients and racial or ethnic minorities and, in conjunction with fixed-dose combination drugs, contributed to the higher rates of errors in nucleoside reverse-transcriptase inhibitor dosing. Understanding the factors related to nucleoside reverse-transcriptase inhibitor dosing errors is an important step in the building of preventive tools.
Definition of nucleoside reverse transcriptase inhibitor in the Legal Dictionary - by Free online English dictionary and encyclopedia. What is nucleoside reverse transcriptase inhibitor? Meaning of nucleoside reverse transcriptase inhibitor as a legal term. What does nucleoside reverse transcriptase inhibitor mean in law?
Definition of reverse transcriptase inhibitor in the Legal Dictionary - by Free online English dictionary and encyclopedia. What is reverse transcriptase inhibitor? Meaning of reverse transcriptase inhibitor as a legal term. What does reverse transcriptase inhibitor mean in law?
Background: Consistent long-term viral suppression has been difficult to achieve in children with human immunodeficiency virus type 1 (HIV-1) infection. We tested the safety and antiviral efficacy of a novel combination consisting of efavirenz, nelfinavir, and one or more nucleoside reverse-transcriptase inhibitors in 57 children previously treated with only nucleoside reverse-transcriptase inhibitors. Methods: The children were monitored for 48 weeks after the initiation of therapy. We assessed plasma concentrations of efavirenz and nelfinavir, plasma HIV-1 RNA levels, and lymphocyte subpopulations. Results: At base line, the 57 HIV-1â€infected children (age range, 3.8 to 16.8 years) had a median of 699 CD4 cells per cubic millimeter and 10,000 copies of HIV-1 RNA per milliliter of plasma. The most common treatment-related effects of at least moderate severity were rash (in 30 percent of children), diarrhea (in 18 percent), neutropenia (in 12 percent), and biochemical abnormalities (in 12 ...
PubMed Central Canada (PMC Canada) provides free access to a stable and permanent online digital archive of full-text, peer-reviewed health and life sciences research publications. It builds on PubMed Central (PMC), the U.S. National Institutes of Health (NIH) free digital archive of biomedical and life sciences journal literature and is a member of the broader PMC International (PMCI) network of e-repositories.
Tang MW., Rhee S-Y., Bertagnolio S., Ford N., Holmes S., Sigaloff KC., Hamers RL., de Wit TFR., Fleury HJ., Kanki PJ., Ruxrungtham K., Hawkins CA., Wallis CL., Stevens W., van Zyl GU., Manosuthi W., Hosseinipour MC., Ngo-Giang-Huong N., Belec L., Peeters M., Aghokeng A., Bunupuradah T., Burda S., Cane P., Cappelli G., Charpentier C., Dagnra AY., Deshpande AK., El-Katib Z., Eshleman SH., Fokam J., Gody J-C., Katzenstein D., Koyalta DD., Kumwenda JJ., Lallemant M., Lynen L., Marconi VC., Margot NA., Moussa S., Ndungu T., Nyambi PN., Orrell C., Schapiro JM., Schuurman R., Sirivichayakul S., Smith D., Zolfo M., Jordan MR., Shafer RW ...
NRTIs (nucleoside reverse transcriptase inhibitors) are active inhibitors of reverse transcriptase found in retroviruses such as the human immunodeficiency virus (HIV). The different nucleoside reverse transcriptase inhibitors may be activated differently but they have the same mechanism of action. NRTIs are activated generally by phosphorylation to the triphosphate form by cellular enzymes. It then competes with cellular triphosphates, which are substrates for proviral DNA by viral reverse transcriptase. Reverse-transcriptase inhibitors (RTIs) are a class of antiretroviral drugs used to treat HIV infection or AIDS, and in some cases hepatitis B. RTIs inhibit activity of reverse transcriptase, a viral DNA polymerase that is required for replication of HIV and other retroviruses.
BACKGROUND: Understanding the selection and decay of drug-resistant HIV-1 variants is important for designing optimal antiretroviral therapy.. OBJECTIVE: To develop a high-throughput, real-time reverse transcriptase (RT) polymerase chain reaction (PCR) assay to quantify non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant variants K103N (AAT or AAC alleles) at frequencies as low as 0.1%, and to apply this to monitor these variants before, during, and after NNRTI therapy.. METHODS: HIV-1 RNA in longitudinal plasma samples obtained from patients starting and stopping NNRTI therapy was converted to cDNA and the target sequence region amplified and quantified by real-time PCR. Approximately 10 copies/reaction provided a template for a second round of PCR using primers that discriminated between the mutant and wild-type alleles. Amplification specificity was confirmed by thermal denaturation analysis.. RESULTS: Frequencies of 103N similar to assay background (0.029%) were observed in ...
Clinical Pharmacokinetics and Antiviral Activity of CC-31244, a Pan-genotypic, Potent Nonnucleoside NS5B Polymerase Inhibitor (NNI) for the Treatment of Hepatitis C ...
Single dose nevirapine (SD NVP) has greatly reduced the rate of mother-to-child transmission (MTCT) of HIV. Non-nucleoside reverse transcriptase inhibitor (NNRTI)-based regimens are recommended for use by the World Health Organization (WHO) in resource-limited settings. However, research suggests that mothers and infants exposed to SD NVP experience higher virologic failure rates when treated with NNRTI-based regimens than their unexposed counterparts. Data show that the use of SD NVP is associated with NNRTI resistance in HIV infected women and infants. The purpose of this trial was to compare and evaluate virologic responses to an NNRTI-based regimen versus a protease-inhibitor (PI)-based regimen in HIV infected infants who had or had not been exposed to SD NVP intrapartum and after birth.. ,,. ,, Participants were enrolled into one of two Cohorts with proposed enrollment into each Cohort of 288 participants. Cohort I participants must have received SD NVP for prevention of MTCT. Cohort II ...
Gastrointestinal side effects of HAART are usually well tolerated and do not contribute to significant treatment discontinuation. However, diarrhea of moderate to severe intensity can occur in patients receiving multi-drug therapy [21-23]. The mechanisms underlying antiretroviral-induced diarrhea are unclear. The intestinal epithelium acts as a highly selective barrier, preventing the passage of toxic molecules and luminal bacterial translocation [24]. The normal barrier function is maintained by steady enterocyte turnover finely regulated by cell proliferation, migration, and apoptosis. Cell-to-cell contacts within the intestinal epithelium structured by a scaffold of tight and adherens junctions, located apically, are further responsible for sealing the intestinal barrier [25-27]. The results of this study suggest that selected antiretroviral drugs influence small intestinal absorptive and secretory functions.. We have assessed intestinal mucosal morphology, permeability changes, and ...
The study is designed to select a dose of GSK1265744 primarily on the basis of antiviral activity and tolerability in HIV-1 infected, antiretroviral naive subjects.. This study consists of two parts:. Induction Phase: Approximately 200 subjects will be randomized (50 subjects in each of the 4 treatment arms). The Induction Phase consists of a 24 week dose-ranging evaluation of GSK1265744 at blinded doses of 10 mg, 30 mg and 60 mg once-daily and a control arm of open-label efavirenz (EFV) 600 mg once daily. The background dual nucleoside reverse transcriptase inhibitor (NRTI) antiretroviral therapy (ART) for all arms will be either abacavir/lamivudine (ABC/3TC) or tenofovir/emtricitabine (TDF/FTC) as selected by the Investigator. Subjects randomized to a GSK1265744 containing arm, who successfully complete 24 weeks on study and demonstrate virologic suppression (defined as having a plasma HIV-1 ribonucleic acid [RNA] ,50 copies per milliliter [c/mL] before Week 24, with no signs of virologic ...
TY - JOUR. T1 - Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. AU - Famiglini, Valeria. AU - La Regina, Giuseppe. AU - Coluccia, Antonio. AU - Masci, Domiziana. AU - Brancale, Andrea. AU - Badia, Roger. AU - Riveira-Muñoz, Eva. AU - Esté, José A.. AU - Crespan, Emmanuele. AU - Brambilla, Alessandro. AU - Maga, Giovanni. AU - Catalano, Myriam. AU - Limatola, Cristina. AU - Formica, Francesca Romana. AU - Cirilli, Roberto. AU - Novellino, Ettore. AU - Silvestri, Romano. PY - 2017/8/10. Y1 - 2017/8/10. N2 - We designed and synthesized a series of chiral indolyarylsulfones (IASs) as new HIV-1 NNRTIs. The new IASs 8-37 showed potent inhibition of the HIV-1 WT NL4-3 strain and of the mutant K103N, Y181C, Y188L, and K103N-Y181C HIV-1 strains. Six racemic mixtures, 8, 23-25, 31, and 33, were separated at semipreparative level into their pure enantiomers. The (R)-8 enantiomer bearing the chiral (α-methylbenzyl) was ...
Panel of prototypical infectious molecular HIV-1 clones containing multiple nucleoside reverse transcriptase inhibitor resistance mutations ...
Pre-incubation of cell-free HIV-1 group M isolates with non-nucleoside reverse transcriptase inhibitors blocks subsequent viral replication in co-cultures of dendritic cells and T cells ...
We restricted our analyses to patients receiving the common ART combination of nucleoside plus non-nucleoside reverse transcriptase inhibitors. We concentrated on this treatment regimen for two major reasons. Firstly, NRTI plus NNRTI regimens are likely to remain popular as first-line therapy because of their demonstrated efficacy, simplicity of therapy, pill number and tolerability [1]. Secondly, NNRTI/NRTI therapy is likely to remain the dominant regimen for first-line therapy in resource-constrained countries. Among the 42 antiretroviral products whose price the Clinton foundation negotiated for resource-constrained countries only two contain PIs [35]. There are 71 countries (including the vast majority of sub-Saharan countries) that can now benefit from this negotiation, representing more than 92% of the people living with HIV globally [36, 37]. It is important to note that, as a general trend, PIs are likely to remain prohibitively expensive for resource-constrained countries in the short ...
Objective: Receptive anal intercourse in both men and women is associated with the highest probability for sexual acquisition of HIV infection. As part of a program to develop an effective prevention strategy, we performed an ex-vivo preclinical evaluation to determine the efficacy of multiple double combinations of maraviroc (MVC) and reverse transcriptase inhibitors (RTIs). Design: The entry inhibitor, MVC, a nucleotide RTI, tenofovir and two non-nucleoside RTIs, UC781 and TMC120 (dapivirine, DPV), were used in double, combinations against a panel of CCR5-using clade B and clade C HIV-1 isolates and against MVC-escape variants. A gel-formulated version of MVC-DPV combination was also tested. Methods: Indicator cells, cocultures of immature dendritic cells with CD4+T cells, and colorectal tissue explants were used to assess antiviral activity of drug combinations. Results: All dual MVC-RTI combinations tested inhibited MVC-sensitive and resistant isolates in cellular and colorectal explants ...
Clinical trial for Vertical infection transmission , Prevention of Perinatal Transmission of HIV-1 Without Nucleoside Reverse Transcriptase Inhibitors
Clinical trial for Vertical infection transmission , Prevention of Perinatal Transmission of HIV-1 Without Nucleoside Reverse Transcriptase Inhibitors
Racivir, also known as PSI-5004; (±)-FTC; RCV, 524W91, is a reverse transcriptase inhibitor potentially for the treatment of HIV infection. 524W91 was anabolized to the active 5-triphosphate in these cells. HBV replication was equally inhibited in cultures incubated with 524W91 when the drug was added 24 h preinfection, at infection, or 24 h postinfection. 524W91 inhibited HBV replication by 50% at less than 20 nM in human hepatocytes.
Learn more about Reverse Transcriptase Inhibitors at Memorial Hospital Coenzyme Q 10 - Possible Benefits and Risks St. Johns...
Learn more about Reverse Transcriptase Inhibitors at Portsmouth Regional Hospital Coenzyme Q 10 - Possible Benefits and Risks ...
Learn more about Reverse Transcriptase Inhibitors at Memorial Hospital Coenzyme Q 10 - Possible Benefits and Risks St. Johns...
Learn more about Reverse Transcriptase Inhibitors at Doctors Hospital of Augusta Coenzyme Q 10 - Possible Benefits and Risks ...
Learn more about Reverse Transcriptase Inhibitors at JFK Medical Center Coenzyme Q 10 - Possible Benefits and Risks St. ...
Learn more about Reverse Transcriptase Inhibitors at Sky Ridge Medical Center Coenzyme Q 10 - Possible Benefits and Risks ...
South Africa (SA) has the highest proportion of HIV-positive people in the world. In 2013, an estimated 10% of the population was HIV-positive, which amounted to 5.26 million people.[1] For adults between the ages of 15 and 49 years, an estimated 15.90% were HIV-positive.[1] However, SA has made positive changes in managing the HIV epidemic. The number of people on antiretroviral therapy (ART) has increased, and there have been fewer AIDS-related deaths from 2005 to 2011.[2]. Antiretrovirals used in the management of HIV. HIV cannot be cured; however, there are several major classes of drugs used in its management. The five classes of drugs used for the management of HIV are entry inhibitors, fusion inhibitors, integrase inhibitors, protease inhibitors and reverse transcriptase inhibitors (nucleoside reverse transcriptase inhibitors and non-nucleoside reverse transcriptase inhibitors).[3] These agents act through various mechanisms to stop the replication of HIV. The recommended regimens for the ...
Pronunciation guide (phonetic spelling and recorded audio) of emtricitabine; tenofovir; rilpivirine, also known as Complera, which is a Top 250 Drug in the drug class of Nucleoside reverse transcriptase inhibitor (NRTI); Non-nucleoside reverse transcriptase inhibitor (NNRTI).
For patients who are starting to take antiretroviral medication (to treat HIV) for the first time, there are now a variety of different medicines which may be taken together as a combination in order to form an effective treatment which suppresses the virus for prolonged periods of time. Currently, national guidelines recommend the use of two different drugs of one type (the nucleoside/ nucleotide reverse transcriptase inhibitors, NRTI often known as nukes) with a third drug from one of two other types (either a nonnucleoside reverse transcriptase inhibitor, known as an NNRTI or nonnuke, or a protease inhibitor, known as a PI) to form a treatment regime of three active drugs. In the UK and Europe, all PIs are given in combination with a small dose of a second PI, ritonavir, which has the effect of boosting the levels of the active PI in the bloodstream. The investigators know from both research studies and patient experience in clinic that a combination of a ritonavirboosted PI with an NNRTI ...
The human immunodeficiency virus (HIV) causes AIDS (acquired immune deficiency syndrome), a disease in which the immune system progressively deteriorates, making sufferers vulnerable to all manner of opportunistic infections. Currently, world-wide there are estimated to be 34 million people living with HIV,
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Effect of a bound non-nucleoside RT inhibitor on the dynamics of wild-type and mutant HIV-1 reverse transcriptase.: HIV-1 reverse transcriptase (RT) is an impor
This study aims at identifying predictors of the treatment decision of German physicians with regard to a non-nucleoside reverse transcriptase inhibitor (NNRTI) or a ritonavir-boosted protease inhibitor (PI/r) -based initial treatment regimen. The study is based on a sub analysis of a nation-wide multi-centre, non-interventional, prospective cohort study. 133 patients were identified, who received antiretroviral first-line therapy. By means of a logistic regression, factors that determine the treatment strategy for treatment-naïve patients were analysed. Compared to patients receiving a NNRTI-based initial regimen, patients treated with PI/r are slightly younger, less educated, in a later stage of HIV and have more concomitant diseases. Regression analysis revealed that being in a later stage of HIV (CDC-C) is significantly associated with a PI/r-based treatment decision. Our analysis is the first study in Germany investigating sociodemographic and disease-specific parameters associated with a NNRTI-
ENGLISH ABSTRACT: Since its discovery in the 1980s, HIV has affected the lives of millions of individuals around the globe. Despite obvious need and an enormous amount of research a cure has remained elusive due to the rapid onset of mutated forms of the virus. However, there has been considerable success in reducing viral levels of infected individuals through the use of highly active antiretroviral therapy (HAART). The first-line regimen HAART mainly targets reverse transcriptase (RT) through the employment of two nucleoside RT inhibitors (NRTIs) and a nonnucleoside RT inhibitor (NNRTI). NNRTIs target an allosteric pocket situated about 10 Å from the catalytic site and cause a conformational change in the enzyme upon binding, leading to the inhibition of viral replication. There are currently 5 FDA approved NNRTIs on the market which successfully inhibit viral replication, but the use of these drugs is becoming limited due to the onset of drug resistant strains of the virus. In light of this ...
Nucleoside reverse transcriptase inhibitors (NRTIs) are mainstay therapeutics for HIV that block retrovirus replication. Alu (an endogenous retroelement that also requires reverse transcriptase for its life cycle)-derived RNAs activate P2X7 and the NLRP3 inflammasome to cause cell death of the retinal pigment epithelium in geographic atrophy, a type of age-related macular degeneration. We found that NRTIs inhibit P2X7-mediated NLRP3 inflammasome activation independent of reverse transcriptase inhibition. Multiple approved and clinically relevant NRTIs prevented caspase-1 activation, the effector of the NLRP3 inflammasome, induced by Alu RNA. NRTIs were efficacious in mouse models of geographic atrophy, choroidal neovascularization, graft-versus-host disease, and sterile liver inflammation. Our findings suggest that NRTIs are ripe for drug repurposing in P2X7-driven diseases ...
This nested case-control study examined relationships between MDR1, CYP2B6, and CYP3A4 variants and hepatotoxicity during antiretroviral therapy with either efavirenz- or nevirapine-containing regimens. Decreased risk of hepatotoxicity was associated with MDR1 3435C→;T (odds ratio, 0.254; P = .021). An interaction between MDR1 and hepatitis B surface antigen status predicted risk with 82% accuracy (P , .001).. ...
SUSTIVA® (sus-TEE-vah) [efavirenz (eh-FAH-vih-rehnz)] capsules and tablets. ALERT: Find out about medicines that should NOT be taken with SUSTIVA.. Please also read the section MEDICINES YOU SHOULD NOT TAKE WITH SUSTIVA.. Read this information before you start taking SUSTIVA (efavirenz). Read it again each time you refill your prescription, in case there is any new information. This leaflet provides a summary about SUSTIVA and does not include everything there is to know about your medicine. This information is not meant to take the place of talking with your doctor.. What is SUSTIVA?. SUSTIVA is a medicine used in combination with other medicines to help treat infection with Human Immunodeficiency Virus type 1(HIV-1), the virus that causes AIDS (acquired immune deficiency syndrome). SUSTIVA is a type of anti-HIV drug called a non-nucleoside reverse transcriptase inhibitor (NNRTI). NNRTIs are not used in the treatment of Human Immunodeficiency Virus type 2 (HIV-2) infection.. SUSTIVA ...
Virtually all the compounds that are currently used, or under advanced clinical trial, for the treatment of HIV infections, belong to one of the following classes: (i) nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs): i.e., zidovudine (AZT), didanosine (ddI), zalcitabine (ddC), stavudine (d4T), lamivudine (3TC), abacavir (ABC), emtricitabine [(-)FTC], tenofovir (PMPA) disoproxil fumarate (ii) non-nucleoside reverse transcriptase inhibitors (NNRTIs): i.e., nevirapine, delavirdine, efavirenz, emivirine (MKC- 442) and (iii) protease inhibitors (PIs): i.e., saquinavir, ritonavir, indinavir, nelfinavir, amprenavir, and lopinavir. In addition to the reverse transcriptase and protease step, various other events in the HIV replicative cycle are potential targets for chemotherapeutic intervention: (i) viral adsorption, through binding to the viral envelope glycoprotein gp120 (polysulfates, polysulfonates, polyoxometalates, zintevir, negatively charged albumins, cosalane analogues) (ii) ...
Anti-HIV drug treatment. Whilst the number of people living with HIV is rising each year, the number of HIV infections that progress to AIDS has dropped dramatically since 1996. This is primarily the result of anti-retroviral therapies, which are available to slow the progress of the virus.. Antiretroviral drugs (ARVs) target essential components of the viral replication cycle and include reverse transciptase (RT) inhibitors, which interfere with the way the virus makes a complementary cDNA copy of its RNA genome, and protease inhibitors, which prevent the virus from cutting up the raw materials it needs to form new viral particles.. Drugs that block RT fall into two categories. These are known as nucleoside and non-nucleoside RT inhibitors. The nucleoside RT inhibitors are structurally very similar to normal DNA bases, but they lack a critical chemical group required to enable a DNA chain to grow. So when the viral RT inserts one of these altered bases into the copy that its making of its ...
Discovery and development of nucleoside and nucleotide reverse-transcriptase inhibitors (NRTIs and NtRTIs) began in the 1980s when the AIDS epidemic hit Western societies. NRTIs inhibit the reverse transcriptase (RT), an enzyme that controls the replication of the genetic material of the human immunodeficiency virus (HIV). The first NRTI was zidovudine, approved by the U.S. Food and Drug Administration (FDA) in 1987, which was the first step towards treatment of HIV. Six NRTI agents and one NtRTI have followed. The NRTIs and the NtRTI are analogues of endogenous 2´-deoxy-nucleoside and nucleotide. Drug-resistant viruses are an inevitable consequence of prolonged exposure of HIV-1 to anti-HIV drugs. In the summer of 1981 the acquired immunodeficiency syndrome (AIDS) was first reported. Two years later the etiological link to AIDS, the human immunodeficiency virus (HIV) was identified. Since the identification of HIV the development of effective antiretroviral drugs and the scientific ...
Learn more about Reverse Transcriptase Inhibitors at Medical City Dallas Coenzyme Q 10 - Possible Benefits and Risks St....
Upon prolonged treatment with various antiretroviral nucleoside analogs such as 3-azido-3-deoxythymidine, 2,3-dideoxyinosine, 2,3-dideoxycytidine, (-)- beta-L-2, 3dideoxy-3thiacytidine and 2,3-didehydro-3-deoxythymidine, selection of human immunodeficiency virus type 1 (HIV-1) strains with mutations in the reverse transcriptase (RT) gene has been reported. We designed a reverse hybridization line probe assay (LiPA) for the rapid and simultaneous characterization of the following variations in the RT gene: M41 or L41; T69, N69, A69, or D69; K70 or R70; L74 or V74; V75 or T75; M184, I184, or V184; T215, Y215, or F215; and K219, Q219, or E219. Nucleotide polymorphisms for codon L41 (TTG or CTG), T69 (ACT or ACA), V75 (GTA or GTG), T215 (ACC or ACT), and Y215 (TAC or TAT) could be detected. In addition to the codons mentioned above, several third-letter polymorphisms in the direct vicinity of the target codons (E40, E42, K43, K73, D76, Q182, Y183, D185, G213, F214, and L214) were found, ...
Nonnucleoside opposite transcriptase (RT) inhibitors (NNRTI) and integrase (IN) strand transfer inhibitors (INSTI) are fundamental the different parts of antiretroviral regimens. of raltegravir (RAL); the RT-K103N mutation experienced no impact. The NNRTI level of resistance mutations experienced no influence on RAL susceptibility. Similarly, the IN-G140S/Q148H mutations experienced no influence on EFV or RPV susceptibility. Nevertheless, both RT-K103N plus IN-G140S/Q148H as well as the RT-E138K plus IN-G140S/Q148H mutant infections experienced significantly greater collapse raises in 50% inhibitory focus (IC50) of EFV than infections carrying an individual NNRTI mutation. Similarly, the RT-E138K plus IN-G140S/Q148H mutant computer virus experienced significantly greater collapse raises in RAL IC50 than that of the IN-G140S/Q148H mutant computer virus. These results claim that relationships between RT and IN mutations IL12RB2 are essential for NNRTI and INSTI level of resistance and viral ...
SUSTIVA® (sus-TEE-vah) [efavirenz (eh-FAH-vih-rehnz)] capsules and tablets. ALERT: Find out about medicines that should NOT be taken with SUSTIVA.. Please also read the section MEDICINES YOU SHOULD NOT TAKE WITH SUSTIVA.. Read this information before you start taking SUSTIVA (efavirenz). Read it again each time you refill your prescription, in case there is any new information. This leaflet provides a summary about SUSTIVA and does not include everything there is to know about your medicine. This information is not meant to take the place of talking with your doctor.. What is SUSTIVA?. SUSTIVA is a medicine used in combination with other medicines to help treat infection with Human Immunodeficiency Virus type 1(HIV-1), the virus that causes AIDS (acquired immune deficiency syndrome). SUSTIVA is a type of anti-HIV drug called a non-nucleoside reverse transcriptase inhibitor (NNRTI). NNRTIs are not used in the treatment of Human Immunodeficiency Virus type 2 (HIV-2) infection.. SUSTIVA ...
Nonnucleoside slow transcriptase inhibitors (NNRTIs) target HIV-1 slow transcriptase (RT) by binding to a pocket in RT thats near, but distinct, through the DNA polymerase energetic site and stop the formation of viral cDNA. set up and demonstrate that legislation of Gag-Pol/Gag-Pol connections is a book target for little molecule inhibitors of HIV-1 creation. Furthermore, these medications can serve as useful probes to help expand understand processes involved with HIV-1 particle set up and maturation. Synopsis HIV-1 encodes invert transcriptase (RT), an enzyme thats essential for computer virus replication. Nonnucleoside invert transcriptase inhibitors (NNRTIs) are allosteric inhibitors from the HIV-1 RT. In HIV-1-contaminated cells NNRTIs stop the RT-catalyzed synthesis of the double-stranded DNA duplicate from the viral genomic RNA, which can be an early part of the computer virus life cycle. Powerful NNRTIs possess the book feature of marketing the interaction between your two RT ...
One of the major problems for AIDS control is the ability of HIV‐1 to develop resistance to antiretroviral compounds used individually or in combination (Balzarini, 1999 and references therein). Sequential monotherapy or combination therapy with several nucleoside RT inhibitors can lead to the appearance of multidrug‐resistant strains. These isolates can accumulate resistance mutations specific for AZT (e.g. M41L, D67N, L210W or T215Y) and other RT inhibitors (e.g. K65R for ddC, L74V for ddI, etc.), which arise during monotherapy. Alternatively, multidrug‐resistant HIV‐1 strains containing the amino acid substitutions A62V, V75I, F77L, F116Y and Q151M may appear under combination therapy with nucleoside RT inhibitors (Shirasaka et al., 1995). Recently, a different multidrug resistance pattern of amino acid substitutions has been observed in a number of patients who were exposed to AZT, ddI, ddC and/or d4T in prolonged therapeutic regimens. Substitution of Thr69 by Ser and insertion of ...
This is a 96 week study to determine if UK- 453,061 in combination with Darunavir /ritonavir and a Nucleos(t)ide Reverse Transcriptase inhibitor is as efficacious, safe and tolerable as etravirine in combination with Darunavir /ritonavir and a Nucleos(t)ide Reverse Transcriptase inhibitor in HIV-1 infected patients who have been previously treated with antiretroviral drugs and have NNRTI resistance mutations ...
Zidovudine (Retrovir). The human immunodeficiency virus replicates by converting its single-standed RNA into double-stranded DNA which is incorporated into host DNA; this crucial conversion, the reverse of the normal cellular transcription of nucleic acids, is accomplished by the enzyme reverse transcriptase. Zidovudine, as the triphosphate, was the first anti-HIV drug to be introduced and has a high affinity for reverse transcriptase. It is integrated by it into the viral DNA chain, causing premature chain termination. The drug must be present continuously to prevent viral alteration of the host DNA, which is permanent once it occurs.. Pharmacokinetics. Zidovudine is well absorbed from the gastrointestinal tract (it is available as capsules and syrup) and is rapidly cleared from the plasma (t1/^ 1 h); concentrations in CSF are approximately half those in plasma. It is also available i.v. for patients temporarily unable to take oral medications. The drug is mainly metabolically inactivated, but ...
TY - JOUR. T1 - Erratum. T2 - Combination nucleoside/nucleotide reverse transcriptase inhibitors for treatment of HIV infection (Expert Opinion on Pharmacotherapy (2012) 13:1(65-79)). AU - Akanbi, M. O.. AU - Scarsi, Kimberly K. AU - Taiwo, B.. AU - Murphy, R. L.. PY - 2015/5/1. Y1 - 2015/5/1. UR - http://www.scopus.com/inward/record.url?scp=84928534685&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=84928534685&partnerID=8YFLogxK. U2 - 10.1517/14656566.2015.1039789. DO - 10.1517/14656566.2015.1039789. M3 - Comment/debate. C2 - 25887247. AN - SCOPUS:84928534685. VL - 16. JO - Expert Opinion on Pharmacotherapy. JF - Expert Opinion on Pharmacotherapy. SN - 1465-6566. IS - 7. ER - ...
A novel HIV-1 inhibitor, 6-(tert-butyl)-4-phenyl-4-(trifluoromethyl)-1H,3H-1,3,5-triazin-2-one (compound 1), was identified from a compound library screened for the ability to inhibit HIV-1 replication. EC50 values of compound 1 were found to range from 107.9 to 145.4 nm against primary HIV-1 clinical isolates. In in vitro assays, HIV-1 reverse transcriptase (RT) activity was inhibited by compound 1 with an EC50 of 4.3 μm. An assay for resistance to compound 1 selected a variant of HIV-1 with a RT mutation (RT(L100I) ); this frequently identified mutation confers mild resistance to non-nucleoside RT inhibitors (NNRTIs). A recombinant HIV-1 bearing RT(L100I) exhibited a 41-fold greater resistance to compound 1 than the wild-type virus. Compound 1 was also effective against HIV-1 with RT(K103N) , one of the major mutations that confers substantial resistance to NNRTIs. Computer-assisted docking simulations indicated that compound 1 binds to the RT NNRTI binding pocket in a manner similar to that ...
Three types of antiretroviral drugs (ARVs) are now used for the treatment of human immunodeficiency virus type 1 (HIV-1) infections, but only reverse transcriptase (RT) inhibitors are readily available to the vast majority of HIV-1-infected individuals in the developing world. The treatment regimen of choice is a combination of a nonnucleoside RT inhibitor (almost exclusively nevirapine [NVP]) and two nucleoside RT inhibitors, i.e., zidovudine (AZT) or stavudine plus lamivudine or didanosine.. In addition to being the backbone of most treatment regimens, NVP is provided as a single dose to block the mother-to-child transmission (MTCT) of HIV-1 in developing countries. In the absence of antiretroviral therapy, the frequency of MTCT is approximately 25 to 48% (2, 36, 38), whereas the administration of a short course of AZT therapy near the end of gestation (7, 8, 49) or the administration of a single dose of NVP at labor can reduce the rate of perinatal transmission to less than 20% (22, 25, 32, ...
FOSTER CITY, Calif. & WHITEHOUSE STATION, N.J.--(BUSINESS WIRE)--Aug. 11, 2006--Gilead Sciences, Inc. (Nasdaq: GILD) and Merck & Co., Inc. (NYSE: MRK) today announced that the companies have established an agreement for the distribution of ATRIPLA(TM) (efavirenz 600 mg/ emtricitabine 200 mg/ tenofovir disoproxil fumarate 300 mg), a once-daily, single tablet regimen for the treatment of HIV-1 infection in adults, in developing countries around the world.. ATRIPLA contains 600 mg of efavirenz, a non-nucleoside reverse transcriptase inhibitor (NNRTI), 200 mg of emtricitabine and 300 mg of tenofovir disoproxil fumarate, both nucleoside reverse transcriptase inhibitors (NRTIs). Efavirenz is marketed by Merck under the tradename Stocrin(R) in all territories outside of the United States, Canada and certain European countries (where it is commercialized by Bristol-Myers Squibb under the tradename Sustiva(R)). Emtricitabine and tenofovir disoproxil fumarate are commercialized by Gilead Sciences under ...
The prices of reverse transcriptase (RT) inhibitors in Thailand have been reduced since December 1, 2001. It is expected that reduction in the price of these inhibitors may influence the drug resistance mutation pattern of HIV-1 among infected people. This study reports the frequency of HIV-1 genetic mutation associated with drug resistance in antiretroviral-treated patients from Thailand. Genotypic resistance testing was performed on samples collected in 2002 from 88 HIV-1 infected individuals. Automated DNA sequencing was used to genotype the HIV-1 polymerase gene isolated from patients plasma. Resistance to protease inhibitors, nucleoside and non-nucleoside reverse transcriptase inhibitors were found in 10 (12%), 42 (48%) and 19 (21%) patients, respectively. The most common drug resistance mutations in the protease gene were at codon 82 (8%), 90 (7%) and 54 (6%), whereas resistant mutations at codon 215 (45%), 67 (40%), 41 (38%) and 184 (27%) were commonly found in the RT gene. This finding
Effect of Food on Absorption of Abacavir and lamivudine Abacavir and lamivudine may be administered with or without food. Administration with a high-fat meal in a single-dose bioavailability trial resulted in no change in AUClast, AUC∞, and Cmax for lamivudine. Food did not alter the extent of systemic exposure to abacavir (AUC∞), but the rate of absorption (Cmax) was decreased approximately 24% compared with fasted conditions (n = 25). These results are similar to those from previous trials of the effect of food on abacavir and lamivudine tablets administered separately.. Specific Populations Patients with Renal Impairment: Abacavir and lamivudine: The effect of renal impairment on the combination of abacavir and lamivudine has not been evaluated (see the U.S. prescribing information for the individual abacavir and lamivudine components).. Patients with Hepatic Impairment: Abacavir and lamivudine: The effect of hepatic impairment on the combination of abacavir and lamivudine has not been ...
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In previously untreated patients, combinations that include efavirenz compare favorably with regimens that include either other nonnucleoside reverse transcriptase inhibitors or components from other antiretroviral classes.. Two parallel randomized, placebo-controlled Phase III studies in antiretroviral-naive adults compared efavirenz with rilpivirine, each in combination with 2 NRTIs (predominantly tenofovir + emtricitabine). By ITT analysis of pooled data from the 2 studies, 82% of efavirenz recipients and 84% of rilpivirine recipients had HIV RNA levels of ,50 copies/mL at 48 weeks; the difference was not statistically significant. In patients with HIV RNA ,100,000 copies/mL, the efavirenz regimen resulted in higher rates of virologic suppression. The mean increase in CD4 count was 176 cells/µL in the efavirenz group (compared with 192 cells/µL in the rilpivirine group).(13) A randomized trial comparing efavirenz with nevirapine, each given with lamivudine + stavudine in initial therapy, ...
Globally of today, acquired immunodeficiency syndrome (AIDS) and malaria are two of the most threatening diseases known to mankind. The World Health Organization estimated that AIDS and malaria together claimed nearly 4 million lives in 2003 and many more were infected by the causative agent human immunodeficiency virus (HIV) and the Plasmodium falciparum (P. falicparum) parasite. Current treatment regims for HIV and P. falicparum infections are undermined by rapid emergence of drug-resistant strains and severe drug side-effects.. A resistance mechanism of the commonly selected K103N RT mutant towards three second generation non-nucleoside RT inhibitors (NNRTIs) is presented based on X-ray structures. Subtle changes in contacts between inhibitor and residue in position 103 aided the design of improved inhibitors. For the PR target, attempts have been made to structurally assist the development of diol-based protease inhibitors (PIs) with the aim of improving the anti-viral potency without ...
Antiretroviral drugs are a very effective therapy against HIV infection. However, the high mutation rate of HIV permits the emergence of variants that can be resistant to the drug treatment. Predicting drug resistance to previously unobserved variants is therefore very important for an optimum medical treatment. In this paper, we propose the use of weighted categorical kernel functions to predict drug resistance from virus sequence data. These kernel functions are very simple to implement and are able to take into account HIV data particularities, such as allele mixtures, and to weigh the different importance of each protein residue, as it is known that not all positions contribute equally to the resistance. We analyzed 21 drugs of four classes: protease inhibitors (PI), integrase inhibitors (INI), nucleoside reverse transcriptase inhibitors (NRTI) and non-nucleoside reverse transcriptase inhibitors (NNRTI). We compared two categorical kernel functions, Overlap and Jaccard, against two well-known
Nevirapine is a non-nucleoside reverse transcriptase inhibitor used to reduce the viral load in HIV infection. Its side effects include hepatotoxicity, gastrointestinal symptoms, and dermatological reaction.1 Efiravenz, another non-nucleoside reverse transcriptase inhibitor, has a similar structure to nevirapine and can cause insomnia and psychotic reactions.1 We report three cases of neuropsychiatric sequelae to nevirapine in patients with HIV infection but no history of mental illness. Medline, Embase, and PsychLIT list no reported cases.. Within two weeks of starting nevirapine a 35 year old man developed low mood and had to stop working because of cognitive impairment and clouding of consciousness. He was admitted after taking an overdose of nevirapine and the treatment was stopped. Five days later, fearing that nursing staff would kill him, he leapt through a third floor window. As the temporal connection to his deterioration was unclear, nevirapine treatment was restarted. After a two week ...
HIV causes a person to become more prone to illness, so infected people need treatment options. However, there is no cure for HIV. To help ease negative symptoms, drugs called anti-retroviral therapy (ART) are available. This treatment is also called high active anti-retroviral therapy (HAART). HAART treatment begins with one non-nucleoside reverse transcriptase inhibitor (NNRTI) and two nucleoside analogue reverse transcriptase inhibitors (NRTIs).[2] The NRTI drug could be named zidovudine (AZT), tenofovir (TDF), andlamivudine (3TC), or emtricitabine (FTC).[3] These drugs slow the progression of the HIV virus in the body.[3] Usually, these treatments consist of a combination of three or more drugs, and each drug performs a different job in fighting the virus. In general, HAART prevents the HIV from multiplying and destroying CD4 cells. CD4 cells are necessary to help protect the body from infections and cancer.[4] Since the HIV virus destroys CD4 cells, it causes people with HIV to be more ...
The introduction of antiretroviral therapy (ART) has intensely reduced HIV-1 associated deaths, mother-to-child HIV-1 transmission, and adult HIV-1 rates. This is as a result of the extensive administration of homogeneous first line regimens that contain two nucleoside reverse transcriptase inhibitors commonly referred to as NRTIs as well as a nonnucleoside RT inhibitor referred to as NNRT. Unfortunately, the long-term success of ART is affected by the development of acquired drug resistance (ADR) and transmitted drug resistance (TDR).. There is an increasing popularity of acquired and transmitted HIV-1 drug resistance. This has consequently become a major obstacle to the success of antiretroviral therapy in the low and middle-income countries that have been hit hardest by the HIV-1 epidemic. To address this issue, experts recommend genotypic drug resistance testing to facilitate the choice of initial ART in areas where there is an increase in transmitted drug resistance. This will also enable ...
Calanolide A is a new non-nucleoside reverse transcriptase inhibitor (NNRTI) derived from a plant found in the Malaysian rain forest. A related compound, calanolide B, also has anti-HIV activity. Both drugs are being developed by Sarawak Pharmaceuticals. A preliminary dosing study among HIV-infected individuals showed a significant antiviral effect compared with placebo.
Emtricitabine is a nucleoside reverse transcriptase inhibitor with an IC50 of 27.7 μM. Buy Reverse Transcriptase inhibitor Emtricitabine from AbMole BioScience.
Etravirine (ETR,[1] brand name Intelence, formerly known as TMC125) is a drug used for the treatment of HIV. Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI). Unlike the currently available agents in the class, resistance to other NNRTIs does not seem to confer resistance to etravirine.[2] Etravirine is marketed by Tibotec, a subsidiary of Johnson & Johnson. In January 2008, the Food and Drug Administration approved its use for patients with established resistance to other drugs, making it the 30th anti-HIV drug approved in the United States and the first to be approved in 2008.[3] It was also approved for use in Canada on April 1, 2008.[4]. Etravirine is licensed in the United States, Canada, Israel, Russia, Australia and the European Union,[5] and is under regulatory review in Switzerland.[6]. ...
TY - JOUR. T1 - Creation of a long-acting nanoformulated 29,39-dideoxy-39-thiacytidine. AU - Guo, Dongwei. AU - Zhou, Tian. AU - Araínga, Mariluz. AU - Palandri, Diana. AU - Gautam, Nagsen. AU - Bronich, Tatiana K. AU - Alnouti, Yazen. AU - McMillan, JoEllyn M. AU - Edagwa, Benson J. AU - Gendelman, Howard Eliot. PY - 2017/3/1. Y1 - 2017/3/1. N2 - Background: Antiretroviral drug discovery and formulation design will facilitate viral clearance in infectious reservoirs. Although progress has been realized for selected hydrophobic integrase and nonnucleoside reverse transcriptase inhibitors, limited success has been seen to date with hydrophilic nucleosides. To overcome these limitations, hydrophobic long-acting drug nanoparticles were created for the commonly used nucleoside reverse transcriptase inhibitor, lamivudine (29,39-dideoxy-39-thiacytidine, 3TC). Methods: A 2-step synthesis created a slow-release long-acting hydrophobic 3TC. Conjugation of 3TC to a fatty acid created a myristoylated ...
One approach that has been used to combat HIV-1 infection is the use of ART, or antiretroviral therapy, and this approach has proven to be effective at reducing viral levels in the blood. ART suppresses HIV-1 viremia to undetectable levels within 12-48 weeks in a majority of patients. This therapy is a cocktail or combination therapy of three or more drugs, including 2 nucleoside-based reverse transcriptase inhibitors (prevents production of the virus genome by inhibiting RNAàDNA transcription), and one or more of the following drugs: non-nucleoside reverse transcriptase inhibitors, membrane fusion inhibitors, viral protease inhibitors, or integrase inhibitors. Each of these drugs targets a specific part of the viral lifecycle, making it unable to replicate and infect other cells. Because each drug is mutually exclusive and targets a different area of the lifecycle, it is unlikely that a virus will develop resistance to all three drugs. Therefore, because the virus does not produce escape ...
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Objective: A novel rapid reverse transcriptase (RT) recombinant HIV-1 drug-susceptibility assay was developed to evaluate resistance to RT inhibitors.. Material and methods: HIV-1 RTs from five treatment-naive and 10 highly active antiretroviral therapy-experienced patients were evaluated. HIV-1 isolates recovered by culturing peripheral blood mononuclear cells from patients were used in the conventional isolate phenotype analysis. Recombinant HIV-1 strains were obtained by cloning the RT gene amplified from the supernatant of HIV-1 cultures in a plasmid carrying the HIV-1 strain HXB2 backbone, and the most represented clone for each virus isolate was then tested for antiviral drug susceptibility in parallel with HIV-1 isolates.. Results: Comparison of conventional virus isolate and the novel recombinant virus phenotypic assays showed a large concordance of results. However, some discrepant results were observed, in that higher drug-resistance levels were detected by the conventional isolate ...
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Anti-viral drug : A Coggle Diagram about ANTI HIV DRUGS (Protease Inhibitors, Nucleoside Reverse Transcriptase Inhibitors, Integrase inhibitor, Entry Inhibitors and Non Nucleoside Reverse Transcriptase Inhibitors) and ANTI HSV DRUGS (Ganciclovir and Acyclovir)
The public health approach to identify antiretroviral therapy failure: High-level nucleoside reverse transcriptase inhibitor resistance among Malawians failing first-line antiretroviral therapy ...
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 ...
... 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. ...
... 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 ...
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 ...
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 ...
... 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 ...
Olivero, Ofelia A. (April 2007). "Mechanisms of genotoxicity of nucleoside reverse transcriptase inhibitors". Environmental and ...
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 ...
... 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 ...
"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. ...
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 ...
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). ...
"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 ...
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 ...
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, ...
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. ...
Menéndez-Arias L (June 2008). "Mechanisms of resistance to nucleoside analogue inhibitors of HIV-1 reverse transcriptase". ...
Trachtenberg, Joel D; Sande Merle A (July 2002). "Emerging resistance to nonnucleoside reverse transcriptase inhibitors: a ...
... 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 ...
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, ...
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 ...
... 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- ...
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 ...
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). ...
... 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 ...
... 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 ...
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) " ...
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. ...
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 & ...
Some notable drugs containing trifluoromethyl groups include efavirenz (Sustiva), an HIV reverse transcriptase inhibitor; ...
Cozaar Losartan angiotensin II receptor antagonist to treat hypertension Sustiva Efavirenz reverse transcriptase inhibitor for ...
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 ...
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 ...
In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodeficiency virus ...
... 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 ...
... 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 ...
... 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 ...
... 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). ...
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 ...
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 ...
... 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 ...
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 ...
"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 ...
... 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 ...
He has shown that adherence to non-nucleoside reverse-transcriptase inhibitor HIV therapy has a linear dose-response pattern. ...
"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 ...
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 ...
Nucleoside analog reverse transcriptase inhibitors, Pyrimidinediones, Organofluorides, Arabinosides, Halohydrins, Hydroxymethyl ...
"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 ...
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 ...
... 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. ...
... 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 ...
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 ...
"Reverse Transcriptase Inhibitors". 0-9. A. B. C. D. E. F. G. H. I. J. K. L. M. N. O. P. Q. R. S. T. U. V. W. X. Y. Z. * 0-9 ...
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. ...
VA » Health Care » HIV » Veterans and Public Home » Treatment » Nucleoside reverse transcriptase inhibitors (NRTIs or nukes) ... It does this by using an enzyme called reverse transcriptase. The NRTIs work because they block that enzyme. Without reverse ...
companys investigational non-nucleoside reverse transcriptase inhibitor. (NNRTI) for the treatment of HIV-1 infection in ... the Companys Investigational Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI), for Treatment of HIV-1 Infection ...
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 ... 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 ...
... 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 ...
From an investigation of lithiation of nucleosides towards a rational design of non-nucleoside reverse transcriptase inhibitors ... From an investigation of lithiation of nucleosides towards a rational design of non-nucleoside reverse transcriptase inhibitors ...
Non-nucleoside reverse transcriptase inhibitors. Recommended change in dose of antiretroviral drug ... Ritonavir-boosted protease inhibitors. Recommended change in dose of antiretroviral drug. Recommended change in dose of ...
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.. ...
"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 ...
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 ...
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 ...
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 ... 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) ...
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) ...
Reverse transcriptase inhibitors. Lamivudine (Epivir). GlaxoSmithKline. 1,000 μM. No. Zidovudine (Retrovir). GlaxoSmithKline. ...
Gupta, Riju, "Nucleoside Reverse Transcriptase Inhibitors Induced Lactic Acidosis" (2021). Tower Health Research Day. 21. https ...
Reverse Transcriptase Inhibitors [‎4]‎. Reverse Transcriptase Polymerase Chain Reaction [‎1]‎. Reverse Transcription [‎1]‎. ...
Non-Nucleoside Reverse Transcriptase Inhibitor. * Non-Nucleoside Reverse Transcriptase Inhibitor * Efavirenz * Etravirine ...
... 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 ...
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 ...
... 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 ...
a. Nucleoside reverse transcriptase inhibitors (NRTIs). Evidence: NRTIs do not appear to have significant risk for interactions ...
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 ... Human endogenous retrovirus-K (HERV-K) reverse transcriptase (RT) structure and biochemistry reveals remarkable similarities to ...
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 ...
Medications for HIV/AIDS (Nucleoside reverse transcriptase inhibitors (NRTIs)). Taking horsetail with NRTIs might reduce the ...
Reverse Transcriptase Inhibitors. Nucleic Acid Synthesis Inhibitors. Enzyme Inhibitors. Molecular Mechanisms of Pharmacological ...
  • 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)
  • 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)
  • 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 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)
  • 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)
  • Replicative fitness costs of nonnucleoside reverse transcriptase inhibitor drug resistance mutations on HIV subtype C. (bvsalud.org)
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • Potent nonnucleoside reverse transcriptase inhibitors target HIV-1 Gag-Pol. (edu.au)
  • 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)
  • 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)
  • 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)
  • Encorafenib (a BCRP inhibitor) may increase the concentration and toxicities of BCRP substrates. (medscape.com)
  • Gupta, Riju, "Nucleoside Reverse Transcriptase Inhibitors Induced Lactic Acidosis" (2021). (towerhealth.org)
  • 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)
  • 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)
  • The twice-weekly dose of RFB (300mg) remains unchanged if the patient is also taking these protease inhibitors. (cdc.gov)
  • 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)
  • 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)
  • 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)
  • 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)
  • HIV reverse transcriptase (RT) is one of the main targets for the action of anti-AIDS drugs. (ox.ac.uk)
  • These analyses suggest that all three drugs interact with HIV-1 RT within the previously defined common binding site for nonnucleoside inhibitors. (nih.gov)