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NucleosidesPurine NucleosidesPyrimidine NucleosidesNucleoside Transport ProteinsEquilibrative Nucleoside Transporter 1ThioinosinePurine-Nucleoside PhosphorylaseGuanosineInosineNucleoside-Diphosphate KinaseUridineRibonucleosidesNucleoside QVirus ReplicationCytidineNucleoside-TriphosphataseEquilibrative-Nucleoside Transporter 2Reverse Transcriptase InhibitorsOrganophosphonatesNucleotidesAdenosineAdenineFormycinsPentosyltransferasesNM23 Nucleoside Diphosphate KinasesInterferonsDrug Resistance, ViralEquilibrative Nucleoside Transport ProteinsZidovudineDeoxyribonucleosidesCell LineAnti-HIV AgentsDeoxyadenosinesHIV-1AcyclovirKineticsDideoxynucleosidesMolecular Sequence DataZalcitabineInterferon Type IDilazepTubercidinPurinesArabinonucleosidesDeoxycytidine KinaseInterferon-alphaThymidineVirusesRNA, ViralDeoxyuridineRibavirinHIV Reverse TranscriptaseAntiviral AgentsVirus DiseasesInterferon-betaNucleoside DeaminasesGuaninePyrimidine PhosphorylasesMyxovirus Resistance ProteinsAmino Acid SequenceDideoxynucleotidesArabinofuranosyluracilThymine NucleotidesLamivudineSubstrate SpecificityMolecular StructureThionucleosidesCytosineMutationRibonucleotidesUridine PhosphorylaseStructure-Activity RelationshipProdrugsBase SequenceViral Plaque AssayStavudineVesicular stomatitis Indiana virusHIV InfectionsHepacivirusDipyridamoleVero CellsGanciclovirAcid Anhydride HydrolasesViral ProteinsAdenosine TriphosphateOrganophosphorus CompoundsCells, CulturedDidanosineImmunity, InnateRibosome Inactivating Proteins, Type 1Thymidine KinaseN-Glycosyl HydrolasesRecombinant ProteinsPyrimidinonesBiological TransportCercopithecus aethiopsModels, MolecularEncephalomyocarditis virusDeoxyguanosineHypoxanthine
AnaloguesAnalogsAnalogNRTIsLamivudineRemdesivirEffective antiviralEfficacyPurineDirect-acting anStructurally relatedAcyclovirTherapeuticProdrugsBroad-spectrumAnalogue reverseProtease InhibitorResistanceTenofovirInhibitionAntibacterialsReverseDrugDrugsClinicalMolnupiravirTreatmentTherapeuticsTherapyAgentsPotentBoneRenalActivityNaturallyCombinationsChemistryPotential
Analogues21
  • Nucleoside analogues are structural analogues of a nucleoside, which normally contain a nucleobase and a sugar. (wikipedia.org)
  • Nucleotide analogues are analogues of a nucleotide, which normally has one to three phosphates linked to a nucleoside. (wikipedia.org)
  • Nucleoside and nucleotide analogues can be used in therapeutic drugs, including a range of antiviral products used to prevent viral replication in infected cells. (wikipedia.org)
  • Nucleotide and nucleoside analogues can also be found naturally. (wikipedia.org)
  • There is a large family of nucleoside analogue reverse transcriptase inhibitors, because DNA production by reverse transcriptase is very different from normal human DNA replication, so it is possible to design nucleoside analogues that are preferentially incorporated by the former. (wikipedia.org)
  • Some nucleoside analogues, however, can function both as NRTIs and polymerase inhibitors for other viruses (e.g., hepatitis B). Less selective nucleoside analogues are used as chemotherapy agents to treat cancer, e.g. gemcitabine. (wikipedia.org)
  • The evolution of antiviral nucleoside analogues: A review for chemists and non-chemists. (wikipedia.org)
  • Antiviral activity of nucleoside analogues against norovirus. (bvsalud.org)
  • The lack of a cell culture has significantly hampered the development of effective therapies against human NoV. Clinically approved nucleoside and non- nucleoside analogues have been used successfully against RNA viruses . (bvsalud.org)
  • In this study, we evaluated the efficacy of four nucleoside analogues (2'-C-MeC, 2'-F-2'-C-MeC, ß-D-N(4)-hydroxycytidine [NHC] and lamivudine ) on Norwalk virus (NV) RNA levels and protein expression in NV replicon -harbouring cells (HG23 cells ), and their efficacy in blocking murine norovirus (MNV) replication in RAW 264.7 cells . (bvsalud.org)
  • Ribavirin is in a class of antiviral medications called nucleoside analogues. (medlineplus.gov)
  • Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogues including lamivudine and zidovudine (components of lamivudine and zidovudine tablets). (nih.gov)
  • Lamivudine is a rare cause of liver test abnormalities or clinically apparent liver injury in patients with HIV infection without hepatitis B. Although several instances of lactic acidosis with hepatic steatosis and liver failure have been reported in patients receiving lamivudine, in all instances other nucleoside analogues more clearly associated with mitochondrial injury [didanosine, stavudine, zalcitrabine, zidovudine] were also being taken. (nih.gov)
  • The active substance in Lamivudine Teva, lamivudine, is an antiviral agent belonging to the class of the nucleoside analogues. (europa.eu)
  • I spent several tears years working with students on using new chemistry to design potential antiviral nucleoside analogues. (davidson.edu)
  • Nucleoside analogues (NAs) are an important class of antiviral and anticancer agents commonly used in the therapy of many different viral infections and cancer conditions. (findaphd.com)
  • Aim To review and evaluate the latest evidence on the safety profiles of the six approved nucleoside analogues. (medscape.com)
  • Yet risks of renal failure and renal replacement therapy were similar in patients treated with nucleoside analogues versus nucleotide analogues in real-life setting. (medscape.com)
  • Long-term use of nucleoside analogues eg entecavir does not increase the risk of other cancers. (medscape.com)
  • Conclusions Long-term safety profile of nucleoside analogues is now better defined with more data from large real-life cohorts and clinical trials with long-term follow-up. (medscape.com)
  • These agents are classified according to their chemical structures: the three nucleoside analogues include lamivudine, telbivudine and entecavir, whereas the two nucleotide analogues include adefovir dipivoxil, tenofovir disoproxil fumarate (TDF), [ 2 ] and the newly approved tenofovir alafenamide (TAF). (medscape.com)
Analogs10
  • Electrophysiological, fluorescence optical, and volume measurements were made to determine the effect of nucleoside analogs on the swelling-dependent chloride current (I Cl ) in NIH 3T3 fibroblasts and in human T cell lymphoma (H9) cells and the cAMP-dependent chloride current in CaCo cells. (biomedcentral.com)
  • The use of nucleoside analogs is a major strategy in the treatment of viral infections. (biomedcentral.com)
  • We show here that nucleoside analogs selectively block I Cl and the regulatory volume decrease (RVD) at concentrations one to two orders of magnitude lower than nucleotides, thus interfering with a vital cell regulatory mechanism at concentrations present in the plasma of patients treated with these drugs. (biomedcentral.com)
  • The mechanism of HBV resistance to nucleoside analogs are described as well as the concept for multiple drug therapy and combination with immunostimulatory approaches. (nih.gov)
  • Both cidofovir and adefovir are nucleoside phosphonate analogs, a class of novel antivirals structurally related to natural nucleotides (Fig. 1 ). (aspetjournals.org)
  • Structure of acyclic nucleoside phosphonate analogs. (aspetjournals.org)
  • Nucleoside analogs ( NA s) are used to treat numerous viral infections and cancer. (plos.org)
  • Nucleoside analogs ( NA s) represent an important drug class for the treatment of viral infections and cancer. (plos.org)
  • von Kleist M, Metzner P, Marquet R, Schütte C (2012) HIV-1 Polymerase Inhibition by Nucleoside Analogs: Cellular- and Kinetic Parameters of Efficacy, Susceptibility and Resistance Selection. (plos.org)
  • The overuse of nucleoside analogs, such as acyclovir (ACV), which suppresses viral DNA polymerase, has led to drug resistance. (molvis.org)
Analog8
  • We show here a novel molecular mechanism by which antiviral drugs of the nucleoside analog family could lead to impairments of the kidney, bone marrow, gastrointestinal, and neuronal functions, and how these side effects could possibly be restricted by the presence of TDP or uridine. (biomedcentral.com)
  • The aim of the present study was to investigate the effect of antiviral drugs from the nucleoside analog family on I Cl . (biomedcentral.com)
  • purine nucleoside analog derived from guanine. (drugs.com)
  • Our model correctly predicts for HIV-1 that resistance against nucleoside analog reverse transcriptase inhibitors (NRTIs) can be conferred by decreasing their incorporation rate, increasing their excision rate, or decreasing their affinity for the polymerase enzyme. (plos.org)
  • Through mathematical modeling, we assess the mechanisms by which HIV-1 can develop resistance against nucleoside analog reverse transcriptase inhibitors (NRTI). (plos.org)
  • It is a nucleoside analog originally developed to treat influenza. (chemistryviews.org)
  • New chemical synthesis of OYA1 as a triphosphate nucleoside analog suitable for in vitro studies on the viral replication mechanism was also described. (cbs42.com)
  • Remdesivir is a nucleoside analog approved by FDA for the treatment of hospitalized patients with COVID-19. (cdc.gov)
NRTIs2
Lamivudine3
  • Lamivudine and zidovudine tablets, a combination of 2 nucleoside analogue reverse transcriptase inibitors, are indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection. (nih.gov)
  • Lamivudine is a nucleoside analogue and reverse transcriptase inhibitor used in the therapy of human immunodeficiency virus (HIV) and hepatitis B virus (HBV) infection. (nih.gov)
  • Lamivudine is currently used in many HAART regimens but is now rarely used to treat hepatitis B because of a high rate of antiviral resistance when it is used as monotherapy as well as the availability of more potent agents with a higher barrier to resistance. (nih.gov)
Remdesivir4
  • Remdesivir , a nucleoside analogue inhibiting viral replication. (tocris.com)
  • One of the therapies we're delivering today is our antiviral treatment for COVID-19, remdesivir. (gilead.com)
  • Thanks to our long-term investment in antivirals, the speed of our response and global collaboration, remdesivir has now reached millions of patients with COVID-19. (gilead.com)
  • Today, Gilead scientists are working to advance additional options for patients with COVID-19, including an oral nucleoside that, once metabolized, works in the same way as remdesivir. (gilead.com)
Effective antiviral1
  • Our studies to date suggest that OYA1 is a highly effective antiviral with long-acting potential due its chemical stability. (cbs42.com)
Efficacy5
  • TAF is a more targeted form of tenofovir that has demonstrated high antiviral efficacy at a dose that is 10 times lower than that of tenofovir DF, as well as an improved renal and bone safety profile. (medscape.com)
  • Cells from all 3 cats were infected with a pathogenic clone of FIV, and in vitro antiviral efficacy of each NRTI was assessed with an FIV p24 antigen capture ELISA. (avma.org)
  • At the highest concentration investigated (10μM), there was no significant difference in antiviral efficacy among the test compounds. (avma.org)
  • Studies also suggest that OYA1 may enhance the efficacy of other antiviral treatments for COVID and Ebola when used as a combination therapy," said Dr. Harold C. Smith , founder and CEO of OyaGen. (cbs42.com)
  • There are considerable differences in efficacy, risk profiles, and use restrictions between the two oral antivirals. (cdc.gov)
Purine3
  • Purine nucleoside phosphorylase (PNP) deficiency, a rare autosomal recessive metabolic disease causes combined immunodeficiency and developmental delay, hypotonia, and spasticity. (frontiersin.org)
  • Purine nucleoside phosphorylase (PNP) deficiency (OMIM 613179) is a rare autosomal recessive metabolic disease leading to combined immunodeficiency and neurological abnormalities, which may include developmental delay, hypotonia, and spasticity ( 1 , 2 ). (frontiersin.org)
  • Purine nucleoside phosphorylase is a ubiquitously expressed enzyme of the purine salvage pathway as is adenosine deaminase, deficiency of which also causes immunodeficiency. (frontiersin.org)
Direct-acting an1
  • The "direct-acting antiviral" or DAA era of HCV treatment has seen the development of several different classes of hepatitis medications. (positivelyaware.com)
Structurally related1
  • Synthetic drug and nucleoside analogue which is structurally related to guanine with antiviral activity. (e-lactancia.org)
Acyclovir2
  • The antiviral drugs AZT and acyclovir are generally used in the treatment of infections with human immunodeficiency virus (HIV) and herpes simplex virus (HSV). (biomedcentral.com)
  • Babies born to mothers infected with genital herpes are often treated with the antiviral drug acyclovir, which can help suppress the virus. (adam.com)
Therapeutic1
  • ROCHESTER, N.Y. , Sept. 18, 2023 /PRNewswire/ -- OyaGen, Inc. Today the company announced publication in Antiviral Research of studies evaluating the mechanism of action of its proprietary COVID therapeutic in preclinical development. (cbs42.com)
Prodrugs2
  • Following a drug repurposing approach, we aimed to investigate and compare the antibacterial and antibiofilm activities of different classes of phosphate prodrugs (HepDirect, cycloSal, SATE and mix SATE) of antiviral and anticancer FDA-approved nucleoside drugs [zidovudine (AZT), floxouridine (FUDR) and gemcitabine (GEM)] against a variety of pathogenic Gram-positive and -negative bacteria. (nih.gov)
  • The prodrugs showed decreased antibacterial activity compared with the parent nucleosides. (nih.gov)
Broad-spectrum2
  • Candidate therapeutics previously shown to be efficacious in non-human primate disease models are based on virus-specific designs and have limited broad-spectrum antiviral potential. (flutrackers.com)
  • OYA1 has broad-spectrum antiviral activity in laboratory-based assays against numerous strains of Coronaviruses and the Ebola virus. (cbs42.com)
Analogue reverse1
  • Therapy should involve combinations of drugs-two nucleoside-analogue reverse-transcriptase inhibitors combined with either a protease inhibitor (PI) or a non-nucleoside-analogue reverse-transcriptase inhibitor. (medscape.com)
Protease Inhibitor1
Resistance4
  • There are, however, several different nucleoside analogue drugs and resistance to one of them is usually overcome by switching to another drug of the same kind (e.g. famciclovir, penciclovir, valaciclovir). (wikipedia.org)
  • Antiviral-resistance mutations often affect more than one drug simultaneously because of similar development pipelines and the ultimate molecular structure of the drug, and combination choices should account for this possibility. (medscape.com)
  • Severe adverse events occur largely when it is withdrawn in patients with chronic hepatitis B or with the development of antiviral resistance. (nih.gov)
  • These elevations appear to be due to a transient flare in the underlying chronic hepatitis B and occur in three situations during and after therapy: upon initiation of therapy (treatment flares), upon development of antiviral resistance (breakthrough flares), and shortly after stopping therapy (withdrawal flares). (nih.gov)
Tenofovir1
  • Hepatitis B is treated with one medication at a time-either an antiviral such as Viread (tenofovir) or Baraclude (entecavir), or with pegylated interferon. (positivelyaware.com)
Inhibition1
  • Experiments including photography of fluorescence in HSV-1g or plaque formation by HSV-1f, western blot assays, real-time RT-PCR assays, cytopathic effect inhibition assays, cytotoxicity assays, and viral absorption and penetration assays were performed to explore the antiviral effect and mechanism of the compounds. (molvis.org)
Antibacterials1
  • Treatment of infections with antibacterials, antifungals, and antivirals. (lu.se)
Reverse2
  • Abacavir tablet, a nucleoside analogue human immunodeficiency virus (HIV-1) reverse transcriptase inhibitor, is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection. (nih.gov)
  • Some, though not all non-nucleoside reverse transcriptase inhibitors (NNRTIs) possess imidazole rings. (i-sis.org.uk)
Drug2
  • Driven by the COVID-19 pandemic and the dire need to discover an antiviral drug, we explored the landscape of the SARS-CoV-2 biomedical publications to identify potential treatments. (jmir.org)
  • Molnupiravir (pictured) is an oral antiviral drug for the treatment of COVID-19. (chemistryviews.org)
Drugs4
  • it is still unclear, however, if this is the exclusive antiviral effect and how different side effects observed both in vitro and in patients treated with these drugs can be explained. (biomedcentral.com)
  • However, various adverse effects may be induced by prolonged administration of antiviral drugs. (aspetjournals.org)
  • Antiviral drugs currently face challenges. (molvis.org)
  • Antiviral drugs do not cure but can control the virus. (msdmanuals.com)
Clinical2
  • Dual antiviral therapy improved the clinical condition and reduced the viral load. (frontiersin.org)
  • Nephrotoxicity is the dose-limiting clinical adverse effect of cidofovir and adefovir, two potent antiviral therapeutics. (aspetjournals.org)
Molnupiravir1
  • Two oral antivirals , Paxlovid (ritonavir-boosted nirmatrelvir) an d molnupiravir, a re now available under Emergency Use Authorization by FDA for treating COVID-19 in outpatients with mild to moderate disease. (cdc.gov)
Treatment1
  • Although treatment is not considered curative, antiviral treatment, monitoring, and liver cancer surveillance can reduce morbidity and mortality. (cdc.gov)
Therapeutics1
  • These data indicate that hOAT1 may significantly contribute to the accumulation of cidofovir and adefovir in renal proximal tubules and, thus, play an active role in the mechanism of nephrotoxicity associated with these antiviral therapeutics. (aspetjournals.org)
Therapy1
  • Successful management of viral infections often requires long-term therapy with highly potent antivirals. (aspetjournals.org)
Agents2
  • It is not yet clear, however, if this is the sole mechanism responsible for the antiviral and/or the numerous side effects observed in patients treated with these agents. (biomedcentral.com)
  • In the absence of a vaccine , antiviral agents could be an effective intervention to control the spread of human NoV in populations at a high risk for NoV disease . (bvsalud.org)
Potent1
  • For the NV replicon , the EC(50) of 2'-C-MeC (1.3 µM) was comparable to the antiviral activity of NHC (1.5 µM) and twofold more potent than 2'-F-2'-C-MeC (3.2 µM). (bvsalud.org)
Bone1
  • Bone toxicity is closely related to nucleoside analogue effect on renal proximal tubular and phosphaturia. (medscape.com)
Renal1
  • Importantly, both hOAT1 and rat renal organic anion transporter 1 (rROAT1) mediated saturable, probenecid-sensitive uptake of cidofovir, adefovir, and other nucleoside phosphonate antivirals. (aspetjournals.org)
Activity1
  • The antiviral activity of 2'-C-MeC against strains of two different NoV genogroups and the low EC(50) suggest that this nucleoside analogue may be effective against the more prevalent GII NoVs. (bvsalud.org)
Naturally1
  • Nucleosides are naturally occurring biological molecules, which are fundamental building blocks of DNA and RNA. (sru.edu)
Combinations1
  • It quickly became apparent that the use of combinations of these direct-acting antivirals (DAAs) could limit emergence of resistant variants while also providing rapid and profound viral suppression. (medscape.com)
Chemistry1
  • I want to get the latest chemistry news from C&EN in my inbox every week. (acs.org)
Potential2
  • To facilitate the identification of potential antivirals, we developed two reporter-expressing ZIKVs, each capable of expressing an enhanced green fluorescent protein or an improved luminescent NanoLuc luciferase. (mdpi.com)
  • At the same time, we are investing in antiviral research and development to help address potential future viral outbreaks and pandemics. (gilead.com)