• Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogs, including VIREAD. (nih.gov)
  • 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)
  • Synthesis of 8-hydroxy and 8-mercapto derivatives of acyclic adenine nucleoside and nucleotide analogs. (cas.cz)
  • The effective HBV NRTIs are nucleoside or nucleotide analogs that can be phosphorylated to their diphosphate or triphosphate active forms by intracellular kinases. (biomedcentral.com)
  • Dual computational and biological assessment of some promising nucleoside analogs against the COVID-19-Omicron variant. (cdc.gov)
  • Evaluation of a series of nucleoside analogs as effective anticoronaviral-2 drugs against the Omicron-B.1.1.529/BA.2 subvariant: A repurposing research study. (cdc.gov)
  • Resistance to multiple nucleoside reverse transcriptase inhibitors (NRTIs) may result from several genotypically distinct pathways, including the Q151M (151 complex), the 69 insertion complex, two distinct thymidine analogue mutational pathways and the K65R mutation. (neb.com)
  • Discovery and development of nucleoside and nucleotide reverse-transcriptase inhibitors (NRTIs and NtRTIs) began in the 1980s when the AIDS epidemic hit Western societies. (wikipedia.org)
  • The NRTIs and the NtRTI are analogues of endogenous 2´-deoxy-nucleoside and nucleotide. (wikipedia.org)
  • NRTIs approved by the FDA are zidovudine, didanosine, zalcitabine, stavudine, lamivudine, abacavir and emtricitabine and the only nucleotide reverse-transcriptase inhibitor (NtRTI) approved is tenofovir (see table 4). (wikipedia.org)
  • NRTIs are analogues of endogenous 2´-deoxy-nucleoside and nucleotide. (wikipedia.org)
  • A variety of enzymes are able to catalyze the final phosphorylation step for NRTIs, including nucleoside diphosphate kinase (NDP kinase), phosphoglycerate kinase, pyruvate kinase and creatine kinase, resulting in formation of respective antivirally active triphosphate analogues. (wikipedia.org)
  • 50 copies per millilitre (c/mL), a standard measure of HIV control, at week 48 when compared to a three-drug regimen of dolutegravir and two nucleoside reverse transcriptase inhibitors (NRTIs), tenofovir disoproxil fumarate/emtricitabine (TDF/FTC), in treatment-naïve, HIV-1 infected adults. (gsk.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)
  • Thus, both nucleoside and nucleotide RT inhibitors (NRTIs) and non-nucleoside RT inhibitors (NNRTI) are extensively used as antiretroviral agents against HBV and HIV infection [ 1 , 2 ]. (biomedcentral.com)
  • In order to remain functional, resistant mutants of HIV-RT need to maintain their capability of incorporating nucleotide at a sufficient rate, as well as to discriminate against NRTIs or improve the excision rate of incorporated NRTIs [ 17 ]. (biomedcentral.com)
  • The use of tenofovir is highly associated with the emergence of mutation K65R, which confers broad resistance to nucleoside/nucleotide analogue reverse transcriptase inhibitors (NRTIs), especially when tenofovir is combined with other NRTIs also selecting for K65R. (unl.pt)
  • Tenofovir disoproxil fumarate (TDF) is an oral prodrug of nucleotide analog tenofovir (TFV, PMPA, 9-[(R)-2-(phosphonomethoxy)propyl]adenine). (biomedcentral.com)
  • 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 (la miv' ue deen) is an L-enantiomer and substituted analogue of cytidine (2',3'-dideoxy-3'-3-thiacytidine: 3TC) and is active against both HIV and HBV in vitro and in vivo. (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)
  • Catalytic mechanism of nucleoside diphosphate kinase investigated using nucleotide analogues, viscosity effects, and X-ray crystallography. (expasy.org)
  • Reference: Nucleoside and nucleotide analogue reverse transcriptase inhibitors: a clinical review of antiretroviral resistance. (neb.com)
  • This review summarizes research advances that further the understanding of nucleoside and nucleotide analogue resistance mutations, and their interplay. (neb.com)
  • The role of INNO-LiPA HBV DR and ultra-deep pyrosequencing in detecting the resistance mutations to nucleoside/nucleotide analogues in viral samples isolated from chronic hepatitis B patients. (genomeweb.com)
  • Through mathematical modeling, we assess the mechanisms by which HIV-1 can develop resistance against nucleoside analog reverse transcriptase inhibitors (NRTI). (plos.org)
  • Kill or corrupt: Mechanisms of action and drug-resistance of nucleotide analogues against SARS-CoV-2. (cdc.gov)
  • They compete with endogenous nucleotides (dNTP/NTP) for incorporation into nascent DNA/RNA and inhibit replication by preventing subsequent primer extension. (plos.org)
  • Since zidovudine was approved in 1987, six nucleosides and one nucleotide reverse-transcriptase inhibitor (NRTI) have been approved by FDA. (wikipedia.org)
  • This study evaluated the safety and efficacy of switching HIV-infected patients with stable viral suppression on nonnucleoside reverse transcriptase inhibitor/nucleoside reverse transcriptase inhibitor (NNRTI/NRTI) therapy to lopinavir/ritonavir (LPV/r) monotherapy. (researchgate.net)
  • Antiretroviral drugs for the treatment of HIV infections belong to six categories: Nucleoside and nucleotide reverse-transcriptase inhibitors, Non-nucleoside reverse-transcriptase inhibitors, protease inhibitors, entry inhibitors, co-receptor inhibitors and integrase inhibitors. (wikipedia.org)
  • The first nucleoside reverse-transcriptase inhibitor with in vitro anti-HIV activity was zidovudine. (wikipedia.org)
  • Activation of nucleoside and nucleotide reverse-transcriptase inhibitors is primarily dependent on cellular entry by passive diffusion or carrier-mediated transport. (wikipedia.org)
  • VIREAD is a nucleotide analog HIV-1 reverse transcriptase inhibitor and an HBV reverse transcriptase inhibitor. (nih.gov)
  • Non-nucleoside reverse transcriptase inhibitor + reverse transcriptase inhibitors (nucleoside + nucleotide analogue). (renalandurologynews.com)
  • FTC 120 mg/TAF 15 mg, in combination with an integrase strand transfer inhibitor (INSTI) or a non-nucleoside reverse transcriptase inhibitor (NNRTI). (hiv.gov)
  • The introduction of nucleotide/nucleoside analogues (NUCs), which block the reverse transcription of HBV polymerase, has markedly improved the prognosis of these patients [ 6 - 9 ]. (e-cmh.org)
  • 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)
  • 6. Cossarizza A., Moyle G. Antiretroviral nucleoside and nucleotide analogues and mitochondria // AIDS. (medline.ru)
  • 15. Moyle G. Clinical manifestations and management of antiretroviral nucleoside analog-related mitochondrial toxicity // Clin. (medline.ru)
  • demonstrated that a 3- susceptible T cells by HIV-bearing dendritic cells could be day course of the nucleoside analog BEA-005 (2,3'-dideoxy-3'- blocked in vitro by the addition of antiretroviral agents to the hydroxymethyl cytidine) prevented either SIV or HIV-2 culture system (4). (cdc.gov)
  • Xanthosine 5-triphosphate (XTP) is a Guanosine triphosphate (GTP) analogue. (ecmdb.ca)
  • Xanthosine 5-triphosphate is an intermediate of the Purine metabolism pathway, a substrate of the enzymes dinucleoside tetraphosphatase (EC 3.6.1.17) and nucleoside-triphosphate pyrophosphatase (EC 3.6.1.19). (ecmdb.ca)
  • Guanylate kinase converts the monophosphate form into diphosphate and triphosphate analogues that inhibit viral DNA replication. (medscape.com)
  • 1994) A simplified procedure for synthesizing nucleoside 1-thiotriphosphates - dATP (alpha)S, dGTP (alpha)S, UTP-alpha-S, and dTTP (alpha)S. (jenabioscience.com)
  • Bepirovirsen, an antisense oligonucleotide therapy aided in long-term prevention of chronic hepatitis B in patients on and not on nucleoside/nucleotide analogues in a Phase II trial. (europeanpharmaceuticalreview.com)
  • Energetic evaluation of hepatocellular carcinoma prediction models within individuals using persistent hepatitis W obtaining nucleotide/nucleoside analogue treatment. (tpca-1inhibitor.com)
  • 2002) pKa perturbation in genomic hepatitis delta virus ribozyme catalysis evidenced by nucleotide analogue interference mapping. (jenabioscience.com)
  • RNA dependent RNA polymerase (RdRp), a critical enzyme in the life cycle of the virus, can be targeted by using nucleotide antivirals thus causing inhibition. (uwo.ca)
  • Triple nucleoside-only regimens: Early virologic failure has been reported in HIV-infected patients. (nih.gov)
  • demonstrated the efficacy of the The role of host defense against HIV is also incompletely nucleotide analog phosphonyl-methoxy-propyladenine (PMPA) delineated. (cdc.gov)
  • 11. Kakuda T.N. Pharmacology of nucleoside and nucleotidereverse transcriptase inhibitor-induced mitochondrial toxicity // Clin.Ther. (medline.ru)
  • Poster session presented at RSC Symposium on Nucleosides and Nucleotides: synthetic and biological chemistry, London, United Kingdom. (qub.ac.uk)
  • Nucleosides are naturally occurring biological molecules, which are fundamental building blocks of DNA and RNA. (sru.edu)
  • Oral anti-HBV nucleoside/nucleotide analogues have been used in pregnant women with high HBV DNA levels to prevent MTCT. (medscape.com)
  • Currently, nucleoside/nucleotide analogue (NA) therapy is the recommended first-line therapy for patients with chronic HBV because it can inhibit viral replication. (medscape.com)
  • The first, and often rate limiting, phosphorylation step (for nucleoside analogues) are most commonly catalyzed by deoxynucleoside kinases. (wikipedia.org)
  • Herpes virus TK, but not host cell TK, uses acyclovir as a purine nucleoside, converting it into acyclovir monophosphate, a nucleotide analogue. (medscape.com)
  • Ribonucleic acid, or RNA, is a nucleic acid polymer consisting of nucleotide monomers, which plays several important roles in the processes of translating genetic information from deoxyribonucleic acid (DNA) into proteins. (wikidoc.org)
  • It is also a substrate for Xanthine triphosphatase, which is a phosphatase that hydrolyzes non-canonical purine nucleotides such as XTP and ITP to their respective diphosphate derivatives. (ecmdb.ca)