R F Schinazi

Summary

Affiliation: Emory University
Country: USA

Publications

  1. pmc Suppression of virus load by highly active antiretroviral therapy in rhesus macaques infected with a recombinant simian immunodeficiency virus containing reverse transcriptase from human immunodeficiency virus type 1
    Thomas W North
    Center for Comparative Medicine, University of California, Davis, CA 95616, USA
    J Virol 79:7349-54. 2005
  2. pmc The Impact of Macrophage Nucleotide Pools on HIV-1 Reverse Transcription, Viral Replication, and the Development of Novel Antiviral Agents
    Christina Gavegnano
    Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30022, USA
    Mol Biol Int 2012:625983. 2012
  3. pmc Residual viremia in an RT-SHIV rhesus macaque HAART model marked by the presence of a predominant plasma clone and a lack of viral evolution
    Robert C Kauffman
    Center for Comparative Medicine, University of California Davis, Davis, California, United States of America Department of Pediatrics, Laboratory of Biochemical Pharmacology, Center for AIDS Research, Emory University School of Medicine, Atlanta, Georgia, United States of America
    PLoS ONE 9:e88258. 2014
  4. pmc Evaluation of single and combination therapies with tenofovir disoproxil fumarate and emtricitabine in vitro and in a robust mouse model supporting high levels of hepatitis B virus replication
    Raymond F Schinazi
    Department of Pediatrics, Emory University School of Medicine, Decatur, GA, USA
    Antimicrob Agents Chemother 56:6186-91. 2012
  5. pmc Use of dietary supplements among people living with HIV/AIDS is associated with vulnerability to medical misinformation on the internet
    Seth C Kalichman
    Department of Psychology, University of Connecticut, 406 Babbidge Road, Storrs, CT 06269, USA
    AIDS Res Ther 9:1. 2012
  6. ncbi request reprint Tissue disposition of 5-o-carboranyluracil--a novel agent for the boron neutron capture therapy of prostate cancer
    Raymond F Schinazi
    Department of Pediatrics, Emory University, Atlanta, Georgia, USA
    Nucleosides Nucleotides Nucleic Acids 23:291-306. 2004
  7. ncbi request reprint Pharmacology of current and promising nucleosides for the treatment of human immunodeficiency viruses
    Raymond F Schinazi
    Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, and Veterans Affairs Medical Center, Decatur, Georgia 30033, USA
    Antiviral Res 71:322-34. 2006
  8. pmc Selection and characterization of HIV-1 with a novel S68 deletion in reverse transcriptase
    Raymond F Schinazi
    Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Veterans Affairs Medical Center, 1670 Clairmont Rd, Medical Research 151H, Decatur, GA 30033, USA
    Antimicrob Agents Chemother 55:2054-60. 2011
  9. pmc HCV drug discovery aimed at viral eradication
    R F Schinazi
    Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Veterans Affairs Medical Center Emory University School of Medicine, Atlanta, GA, USA
    J Viral Hepat 17:77-90. 2010
  10. ncbi request reprint Cell-based and animal models for hepatitis B and C viruses
    R F Schinazi
    Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA
    Antivir Chem Chemother 10:99-114. 1999

Research Grants

  1. HIV DART:Frontiers in Drug Development for ARV Therapies
    RAYMOND SCHINAZI; Fiscal Year: 2007
  2. NUCLEOSIDES WITH DUAL ANTI-HIV AND HBV ACTIVITY
    RAYMOND SCHINAZI; Fiscal Year: 2007

Detail Information

Publications108 found, 100 shown here

  1. pmc Suppression of virus load by highly active antiretroviral therapy in rhesus macaques infected with a recombinant simian immunodeficiency virus containing reverse transcriptase from human immunodeficiency virus type 1
    Thomas W North
    Center for Comparative Medicine, University of California, Davis, CA 95616, USA
    J Virol 79:7349-54. 2005
    ..These results mimic HAART of HIV-1-infected humans. The RT-SHIV/rhesus macaque model should be useful for studies of tissue reservoirs and sites of residual replication that are not possible or practical with humans...
  2. pmc The Impact of Macrophage Nucleotide Pools on HIV-1 Reverse Transcription, Viral Replication, and the Development of Novel Antiviral Agents
    Christina Gavegnano
    Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30022, USA
    Mol Biol Int 2012:625983. 2012
    ....
  3. pmc Residual viremia in an RT-SHIV rhesus macaque HAART model marked by the presence of a predominant plasma clone and a lack of viral evolution
    Robert C Kauffman
    Center for Comparative Medicine, University of California Davis, Davis, California, United States of America Department of Pediatrics, Laboratory of Biochemical Pharmacology, Center for AIDS Research, Emory University School of Medicine, Atlanta, Georgia, United States of America
    PLoS ONE 9:e88258. 2014
    ..Therefore, this model may be ideal for testing HIV-1 eradication strategies...
  4. pmc Evaluation of single and combination therapies with tenofovir disoproxil fumarate and emtricitabine in vitro and in a robust mouse model supporting high levels of hepatitis B virus replication
    Raymond F Schinazi
    Department of Pediatrics, Emory University School of Medicine, Decatur, GA, USA
    Antimicrob Agents Chemother 56:6186-91. 2012
    ..TDF-(-)-FTC combination therapy provides more effective HBV suppression than therapy with each drug alone...
  5. pmc Use of dietary supplements among people living with HIV/AIDS is associated with vulnerability to medical misinformation on the internet
    Seth C Kalichman
    Department of Psychology, University of Connecticut, 406 Babbidge Road, Storrs, CT 06269, USA
    AIDS Res Ther 9:1. 2012
    ..abstract:..
  6. ncbi request reprint Tissue disposition of 5-o-carboranyluracil--a novel agent for the boron neutron capture therapy of prostate cancer
    Raymond F Schinazi
    Department of Pediatrics, Emory University, Atlanta, Georgia, USA
    Nucleosides Nucleotides Nucleic Acids 23:291-306. 2004
    ..CU was found to be the most suitable compound for further development to treat prostate cancer...
  7. ncbi request reprint Pharmacology of current and promising nucleosides for the treatment of human immunodeficiency viruses
    Raymond F Schinazi
    Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, and Veterans Affairs Medical Center, Decatur, Georgia 30033, USA
    Antiviral Res 71:322-34. 2006
    ....
  8. pmc Selection and characterization of HIV-1 with a novel S68 deletion in reverse transcriptase
    Raymond F Schinazi
    Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Veterans Affairs Medical Center, 1670 Clairmont Rd, Medical Research 151H, Decatur, GA 30033, USA
    Antimicrob Agents Chemother 55:2054-60. 2011
    ..These data indicate that the novel S68Δ is a previously unrecognized deletion that may represent an important factor in NRTI multidrug resistance treatment strategies...
  9. pmc HCV drug discovery aimed at viral eradication
    R F Schinazi
    Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Veterans Affairs Medical Center Emory University School of Medicine, Atlanta, GA, USA
    J Viral Hepat 17:77-90. 2010
    ....
  10. ncbi request reprint Cell-based and animal models for hepatitis B and C viruses
    R F Schinazi
    Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA
    Antivir Chem Chemother 10:99-114. 1999
    ..The characterization of well-defined viral targets coupled with improved molecular diagnostic technologies have illuminated this field...
  11. ncbi request reprint Early detection of mixed mutations selected by antiretroviral agents in HIV-infected primary human lymphocytes
    R F Schinazi
    Department of Veterans Affairs, Decatur, GA, USA
    Antivir Chem Chemother 12:61-5. 2001
    ..Rapid genotyping analysis revealed the different kinetics and mutations obtained by in vitro selection in HIV-infected cells exposed to nucleoside analogues and protease inhibitors...
  12. ncbi request reprint Treatment of isografted 9L rat brain tumors with beta-5-o-carboranyl-2'-deoxyuridine neutron capture therapy
    R F Schinazi
    Department of Pediatrics, Emory University School of Medicine, Atlanta, Georgia 30322, USA
    Clin Cancer Res 6:725-30. 2000
    ..036), which may correlate with the decreased tumor selectivity for D-CDU observed at the higher dose. Additional pharmacodynamic studies are warranted to determine optimal dosing strategies for D-CDU...
  13. pmc DPC 817: a cytidine nucleoside analog with activity against zidovudine- and lamivudine-resistant viral variants
    Raymond F Schinazi
    Veterans Affairs Medical Center, Atlanta, Georgia 30033, USA
    Antimicrob Agents Chemother 46:1394-401. 2002
    ..Together, these properties suggest that DPC 817 may be useful as a component of HAART regimens in individuals with resistance to older NRTI agents...
  14. ncbi request reprint Correlation of human immunodeficiency virus type 1 RNA levels in blood and the female genital tract
    C E Hart
    Division of AIDS, STD, and TB Laboratory Research, Centers for Disease Control and Prevention, Atlanta, Georgia 30333, USA
    J Infect Dis 179:871-82. 1999
    ..These findings suggest that factors that lower blood plasma virus load may also reduce the risk of perinatal and female-to-male heterosexual transmission by lowering vaginal virus load...
  15. ncbi request reprint Development of a pharmacodynamic model for HIV treatment with nucleoside reverse transcriptase and protease inhibitors
    Selwyn J Hurwitz
    Department of Pediatrics, Center for AIDS Research and Laboratory of Biochemical Pharmacology, Emory University School of Medicine, Atlanta 30332, GA, USA
    Antiviral Res 56:115-27. 2002
    ..However, the model overestimated the efficacy of highly effective drug combinations where all three agents are combined as in highly active anti-retroviral therapy...
  16. pmc Antiviral and cellular metabolism interactions between Dexelvucitabine and lamivudine
    Brenda I Hernandez-Santiago
    Veterans Affairs Medical Center, Medical Research 151H, 1670 Clairmont Road, Decatur, GA 30033, USA
    Antimicrob Agents Chemother 51:2130-5. 2007
    ..However, it may be necessary to decrease the dose of 3TC for this combination to prove effective...
  17. ncbi request reprint Nucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase
    Prem L Sharma
    Department of Pediatrics, Laboratory of Biochemical Pharmacology, Emory University School of Medicine, Atlanta, Georgia, USA
    Curr Top Med Chem 4:895-919. 2004
    ....
  18. ncbi request reprint Potent antiviral effect of reverset in HIV-1-infected adults following a single oral dose
    Lieven J Stuyver
    Pharmasset, Inc, Tucker, GA, USA
    Antivir Ther 9:529-36. 2004
    ..A single 10 mg RVT dose resulted in a viral load drop of 0.61 +/- 0.05 log10 providing evidence that a viral strain with the indicated genotype is susceptible to RVT...
  19. pmc Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate
    Johan Lennerstrand
    Laboratory of Biochemical Pharmacology, Emory University Veterans Affairs Medical Center, 1670 Clairmont Rd, Medical Research 151 H, Decatur, GA 30033, USA
    Antimicrob Agents Chemother 51:2078-84. 2007
    ....
  20. pmc Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals
    Selwyn J Hurwitz
    Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, Georgia 30322, USA
    Antimicrob Agents Chemother 54:1248-55. 2010
    ..Coadministration of AMDX with ZDV did not significantly change either of the plasma PK parameters or percent recovery in the urine of AMDX, DXG, or ZDV/GZDV. Larger studies with AMDX/ZDV, with a longer duration, are warranted...
  21. ncbi request reprint Cellular replication of human immunodeficiency virus type 1 occurs in vaginal secretions
    T V Ellerbrock
    Division of HIV AIDS Prevention, Surveillance, and Epidemiology, National Center for HIV, STD, and TB Prevention, National Center for Infectious Diseases, Centers for Disease Control and Prevention, Atlanta, GA 30333, USA
    J Infect Dis 184:28-36. 2001
    ..These findings indicate that cellular replication of HIV-1 occurs in vaginal secretions and can result in a virus population with important differences from that in blood...
  22. pmc Combinations of isoprinosine and 3'-azido-3'-deoxythymidine in lymphocytes infected with human immunodeficiency virus type 1
    R F Schinazi
    Veterans Administration Medical Center, Decatur, Georgia 30033
    Antimicrob Agents Chemother 32:1784-7. 1988
    ..The in vitro results indicate that this combination did not decrease the efficacy of AZT or exacerbate virus replication...
  23. ncbi request reprint Polyoxometalate HIV-1 protease inhibitors. A new mode of protease inhibition
    D A Judd
    Contribution from the Department of Chemistry, Emory University, Atlanta, Georgia 30322, USA
    J Am Chem Soc 123:886-97. 2001
    ..1 +/- 0.5 and 4.1 +/- 1.8 nM in 0.1 and 1.0 M NaCl, respectively) and inhibition is noncompetitive (k(cat) but not K(m) is affected by the POM concentration)...
  24. ncbi request reprint Treatment modalities for hepatitis B viral infection and resistance to antiviral therapy
    S B Pai
    Veterans Affairs Medical Center, Emory University School of Medicine, Decatur, GA 30033, USA
    Panminerva Med 45:165-73. 2003
    ..With the combination of a number of treatment protocols, it should be possible to bring down the viral load to undetectable levels and minimize the risk of generating mutations that confer resistance to the therapeutic agent...
  25. pmc Comparative analysis of in vitro processivity of HIV-1 reverse transcriptases containing mutations 65R, 74V, 184V and 65R+74V
    Prem L Sharma
    Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, United States
    Antiviral Res 83:317-23. 2009
    ..Since these surprising biochemical results cannot explain the clinical phenotype, a hypothesis is presented to explain the discrepancy and suggest new approaches for future testing...
  26. ncbi request reprint Synthesis and evaluation of 2'-substituted cyclobutyl nucleosides and nucleotides as potential anti-HIV agents
    Yongfeng Li
    Department of Chemistry, Emory University, Atlanta, GA 30322, USA
    Bioorg Med Chem Lett 17:3398-401. 2007
    ..7, 6.9 microM), but also against the M184I and M184V mutants (IC(50)=6.1, 6.9 microM) in cell-free assays...
  27. pmc Development of an optimized dose for coformulation of zidovudine with drugs that select for the K65R mutation using a population pharmacokinetic and enzyme kinetic simulation model
    Selwyn J Hurwitz
    Veterans Affairs Medical Center, Medical Research 151H, 1670 Clairmont Road, Decatur, GA 30033, USA
    Antimicrob Agents Chemother 52:4241-50. 2008
    ..i.d., indicating that q.d. dosing with ZDV should be avoided. These in silico predictions suggest that 200 mg ZDV b.i.d. is an efficacious and safe dose that could delay the emergence of the K65R mutation...
  28. ncbi request reprint Development of a population simulation model for HIV monotherapy virological outcomes using lamivudine
    Selwyn J Hurwitz
    Center for AIDS Research and Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA, USA
    Antivir Chem Chemother 18:329-41. 2007
    ..Therefore, once parameter and variance distributions are standardized, this modelling approach could be helpful in planning clinical trials and predicting the antiviral contribution of each agent in a HAART modality...
  29. ncbi request reprint Replication-dependent 65R-->K reversion in human immunodeficiency virus type 1 reverse transcriptase double mutant K65R + L74V
    Prem L Sharma
    Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine Veterans Affairs Medical Center, Decatur, GA 30033, USA
    Virology 321:222-34. 2004
    ..A similar phenomenon may occur in vivo, which may have implications for treatment management strategies...
  30. ncbi request reprint Biologic properties of human herpesvirus 7 strain SB
    J B Black
    Centers for Disease Control and Prevention, Atlanta, GA 30333, USA
    Virus Res 52:25-41. 1997
    ..A generalized increase in host cell protein synthesis was also observed in virus-infected cells similar to that seen in CBL infected with human herpesvirus 6...
  31. pmc Inhibition of B virus (Macacine herpesvirus 1) by conventional and experimental antiviral compounds
    P W Krug
    Viral Immunology Center, Georgia State University, P O Box 4118, Atlanta, GA 30302, USA
    Antimicrob Agents Chemother 54:452-9. 2010
    ..Further, the considerably higher potency of FEAU (2'-fluoro-5-ethyl-Ara-U) than of conventional antiviral drugs argues for its compassionate use in advanced human B virus infections...
  32. ncbi request reprint Mechanism of antiviral activities of 3'-substituted L-nucleosides against 3TC-resistant HBV polymerase: a molecular modelling approach
    Youhoon Chong
    Department of Pharmaceutical and Biomedical Sciences, College of Pharmacy, University of Georgia, Athens, GA, USA
    Antivir Chem Chemother 14:309-19. 2003
    ....
  33. ncbi request reprint N4-acyl-modified D-2',3'-dideoxy-5-fluorocytidine nucleoside analogues with improved antiviral activity
    Junxing Shi
    Pharmasset, Inc, Tucker, GA, USA
    Antivir Chem Chemother 14:81-90. 2003
    ....
  34. ncbi request reprint Characterization of hepatitis B virus inhibition by novel 2'-fluoro-2',3'-unsaturated beta-D- and L-nucleosides
    S Balakrishna Pai
    Veterans Affairs Medical Center, Decatur, GA, USA
    Antivir Chem Chemother 16:183-92. 2005
    ..This class of nucleosides, which exhibit potent antiviral activity and a favourable safety profile, have potential for the treatment of HBV infections and warrant further development...
  35. ncbi request reprint PAMAM dendrimers and branched polyethyleneglycol (nanoparticles) prodrugs of (-)-beta-D-(2R, 4R)-dioxolane-thymine (DOT) and their anti-HIV activity
    Yuzeng Liang
    The University of Georgia College of Pharmacy, Athens, GA, USA
    Antivir Chem Chemother 17:321-9. 2006
    ..Unfortunately, the PAMAM dendrimers also exhibited increased cytotoxicity. Anti-HIV activity of PEG-DOT conjugates was found to be lower than that of DOT...
  36. pmc Emergence of a novel mutation in the FLLA region of hepatitis B virus during lamivudine therapy
    S Balakrishna Pai
    Veterans Affairs Medical Center, Medical Research 151 H, 1670 Clairmont Road, Decatur, Georgia 30033, USA
    Antimicrob Agents Chemother 49:2618-24. 2005
    ..The resistance profile was comparable to that of the previously reported rtL180 M/M204I-containing virus. These observations were further confirmed by generation of stable cultures transfected with the mutant virus...
  37. ncbi request reprint All-oral, interferon-free treatment for chronic hepatitis C: cost-effectiveness analyses
    L M Hagan
    Department of Pediatrics, Laboratory of Biochemical Pharmacology, Center for AIDS Research, Emory University School of Medicine, Atlanta, GA, USA Emory University Rollins School of Public Health, Atlanta, GA, USA Veterans Affairs Medical Center, Decatur, GA, USA
    J Viral Hepat 20:847-57. 2013
    ..Quality-adjusted life years gained per dollar spent were maximized in younger treatment cohorts. Using this model, the degree of cost-effectiveness depended on the WTP threshold and the final cost set for approved drug combinations...
  38. ncbi request reprint Nomenclature for antiviral-resistant human hepatitis B virus mutations in the polymerase region
    L J Stuyver
    Veterans Affairs Medical Center, Decatur, GA, USA
    Hepatology 33:751-7. 2001
    ..The new consensus rt domain numbering system is genotype independent and allows investigators to number any previously and newly discovered antiviral-related amino acid change in a standardized manner...
  39. pmc Pharmacology and pharmacokinetics of the antiviral agent beta-D-2',3'-dideoxy-3'-oxa-5-fluorocytidine in cells and rhesus monkeys
    Brenda I Hernandez-Santiago
    Department of Pediatrics, Emory School of Medicine Veterans Affairs Medical Center, Medical Research 151H, 1670 Clairmont Rd, Decatur, Georgia 30033, SUA
    Antimicrob Agents Chemother 49:2589-97. 2005
    ..These results suggest that further safety and pharmacological studies are warranted to assess the potential of this nucleoside for the treatment of HIV- and HBV-infected individuals...
  40. pmc Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys
    Ghazia Asif
    Department of Pediatrics, Emory University School of Medicine, Atlanta, Georgia, USA
    Antimicrob Agents Chemother 51:2424-9. 2007
    ..The potent antiretroviral activity of D-DOT against a lamivudine- and zidovudine-resistant HIV-1 mutant, together with an excellent pharmacokinetic profile for rhesus monkeys, suggest that further development is warranted...
  41. ncbi request reprint Short communication cellular pharmacology of 9-(beta-D-1,3-dioxolan-4-yl) guanine and its lack of drug interactions with zidovudine in primary human lymphocytes
    Brenda I Hernandez-Santiago
    Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Veterans Affairs Medical Center, Decatur, GA 30033, USA
    Antivir Chem Chemother 18:343-6. 2007
    ..Taken together, these results suggest that an appropriately designed DXG prodrug could be given once a day and that co-formulation with ZDV might be a possibility...
  42. ncbi request reprint Hepatitis B virus resistance to lamivudine and its clinical implications
    Xuefeng Liu
    Veterans Affairs Medical Center, Department of Pediatrics, Emory University School of Medicine, GA, USA
    Antivir Chem Chemother 13:143-55. 2002
    ..Ultimately, once several antiviral agents are approved, combination strategy is likely to be incorporated in antiviral treatment for chronic HBV to suppress, prevent or minimize the emergence of resistant virus...
  43. ncbi request reprint Comparative pharmacokinetics of Racivir, (+/-)-beta-2',3'-dideoxy-5-fluoro-3'-thiacytidine in rats, rabbits, dogs, monkeys and HIV-infected humans
    Selwyn J Hurwitz
    Department of Pediatrics, Emory University School of Medicine and Veterans Affairs Medical Center, Decatur, GA, USA
    Antivir Chem Chemother 16:117-27. 2005
    ....
  44. pmc Metabolism of the anti-hepatitis C virus nucleoside beta-D-N4-hydroxycytidine in different liver cells
    Brenda I Hernandez-Santiago
    Department of Pediatrics, Emory School of Medicine, and Veterans Affairs Medical Center, Decatur, Georgia 30033, USA
    Antimicrob Agents Chemother 48:4636-42. 2004
    ..Studies using monkey and human whole blood demonstrated more-rapid deamination and oxidation in monkey cells than in human cells, suggesting that NHC may not persist long enough in plasma to be delivered to liver cells...
  45. pmc Pharmacokinetics of the antiviral agent beta-L-3'-fluoro-2',3'-didehydro-2',3'-dideoxycytidine in rhesus monkeys
    Ghazia Asif
    Department of Pediatrics, Emory University, Atlanta, Georgia, USA
    Antimicrob Agents Chemother 49:560-4. 2005
    ..49), suggesting that further development of this compound may warrant other approaches, such as development of a prodrug to improve its oral absorption...
  46. ncbi request reprint Synthesis of enantiomerically pure D-FDOC, an anti-HIV agent
    Shuli Mao
    Department of Chemistry, Emory University, 403 Cherry Logan Emerson Hall, 1521 Dickey Drive, Atlanta, GA 30322, USA
    Bioorg Med Chem Lett 14:4991-4. 2004
    ..In addition, conditions were developed that allowed the unwanted butyrate ester of the L-enantiomer of FDOC to be racemized. This material could then be recycled in future resolutions...
  47. pmc Antiviral activity and pharmacokinetics of 1-(2,3-dideoxy-2-fluoro-beta-L-glyceropent-2-enofuranosyl)cytosine
    Huachun Chen
    Department of Pediatrics, Emory University and Veterans Affairs Medical Center, Decatur, Georgia 30033, USA
    Antimicrob Agents Chemother 47:1922-8. 2003
    ..Based upon these observations, further testing to develop this agent for treatment of HIV and HBV infections is warranted...
  48. pmc Antiviral activities and cellular toxicities of modified 2',3'-dideoxy-2',3'-didehydrocytidine analogues
    Lieven J Stuyver
    Veterans Affairs Medical Center and Department of Pediatrics, Emory University School of Medicine, Decatur, Georgia 30033, USA
    Antimicrob Agents Chemother 46:3854-60. 2002
    ..08 micro M) and lamivudine-resistant HIV-1 (EC(90) = 0.15 micro M) is markedly reduced by introduction of a 3'-fluorine in the sugar (EC(90)s of compound 2a, 37.5 and 494 micro M, respectively)...
  49. ncbi request reprint Mutations in the conserved woodchuck hepatitis virus polymerase FLLA and YMDD regions conferring resistance to lamivudine
    Kathleen M Tatti
    Laboratory of Biochemical Pharmacology, Department of Pediatrics, Veterans Affairs Medical Center and Emory University, Medical Research 151H, 1670 Clairmont Road, Decatur, GA 30033, USA
    Antiviral Res 55:141-50. 2002
    ..These results further illustrate the utility of the WHV/woodchuck model to studies of HBV-drug resistance...
  50. ncbi request reprint Anti-hepatitis C virus activity of novel beta-d-2'-C-methyl-4'-azido pyrimidine nucleoside phosphoramidate prodrugs
    Ramu Rondla
    Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine and Veterans Affairs Medical Center, Atlanta, GA, USA
    Antivir Chem Chemother 20:99-106. 2009
    ..In an effort to discover new and more potent anti-HCV agents, we envisioned synthesizing nucleoside analogues by combining the 2'-C-methyl-moiety with the 4'-azido-moiety into one molecule...
  51. pmc Simultaneous quantification of 9-(beta-D-1,3-dioxolan-4-yl)guanine, Amdoxovir and Zidovudine in human plasma by liquid chromatography-tandem mass spectrometric assay
    Emilie Fromentin
    Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Veterans Affairs Medical Center, Decatur, GA 30033, USA
    J Chromatogr B Analyt Technol Biomed Life Sci 877:3482-8. 2009
    ..The analytes were chemically stable under all relevant conditions and the method was successfully applied for the analysis of plasma samples from HIV-infected persons treated with combinations of DAPD and ZDV...
  52. pmc Synthesis, antiviral activity, and stability of nucleoside analogs containing tricyclic bases
    Franck Amblard
    Department of Pediatrics, Center for AIDS Research, Veterans Affairs Medical Center, Laboratory of Biochemical Pharmacology, Emory University School of Medicine, Atlanta, GA 30033, USA
    Eur J Med Chem 44:3845-51. 2009
    ..Their in vitro activity against HIV and HCV was evaluated and correlated to their ability to degrade to their purine counterpart...
  53. pmc Long-term exposure to AZT, but not d4T, increases endothelial cell oxidative stress and mitochondrial dysfunction
    Erik R Kline
    Division of Pulmonary, Allergy and Critical Care Medicine, Emory University School of Medicine Atlanta VA Medical Center, Atlanta, GA 30033, USA
    Cardiovasc Toxicol 9:1-12. 2009
    ..Endothelial cells are more susceptible to AZT-induced toxicity than HepG2 cells, and AZT caused greater endothelial dysfunction than d4T because of its pro-oxidative effects...
  54. pmc Combinations of 2'-C-methylcytidine analogues with interferon-alpha2b and triple combination with ribavirin in the hepatitis C virus replicon system
    Leda Bassit
    Department of Pediatrics, Emory University School of Medicine, Veterans Affairs Medical Centre, Decatur, Georgia 30033, USA
    Antivir Chem Chemother 19:25-31. 2008
    ....
  55. pmc Simultaneous quantification of intracellular natural and antiretroviral nucleosides and nucleotides by liquid chromatography-tandem mass spectrometry
    Emilie Fromentin
    Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, Georgia 30332, USA
    Anal Chem 82:1982-9. 2010
    ..This novel method demonstrated optimal sensitivity (limit of detection 1-10 nM for various analytes), specificity, and reproducibility to successfully measure NRTI-TP and dNTP in human PBM cells and macrophages...
  56. ncbi request reprint Synthesis and anti-hepatitis C virus activity of nucleoside derivatives of N3, 5'-anhydro-4-(beta-D-ribofuranosyl)-8-aza-purin-2-ones
    Abdalla E A Hassan
    Department of Chemical Sciences, Pharmasset, Inc, Tucker, Georgia, USA
    Nucleosides Nucleotides Nucleic Acids 24:961-4. 2005
    ..A series of N3, 5-Anhydro-4-(beta-D-ribofuranosyl)-8-azapurin-2-ones were prepared in multistep reactions from uridine as potential anti-hepatitis C virus (HCV) agents. The synthetic details as well as biological evaluations are discussed...
  57. pmc Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys
    Ghazia Asif
    Veterans Affairs Medical Center, Medical Research 151H, Decatur, GA 30033, USA
    Antimicrob Agents Chemother 51:2877-82. 2007
    ..Further studies are warranted to improve the oral bioavailability and reduce the deamination of PSI-6130 in order to explore the potential of this drug for the treatment of HCV-infected individuals...
  58. ncbi request reprint Synthesis and in vitro anti-HCV activity of beta-D- and 1-2'-deoxy-2'-fluororibonucleosides
    Junxing Shi
    Pharmasset, Inc, Tucker, GA, USA
    Nucleosides Nucleotides Nucleic Acids 24:875-9. 2005
    ..All the L-forms of the analogues were devoid of anti-HCV activity. None of the compounds showed anti-BVDV activity, suggesting that the BVDV system cannot reliably predict anti-HCV activity in vitro...
  59. pmc Facile purification of honokiol and its antiviral and cytotoxic properties
    Franck Amblard
    Department of Pediatrics and Dermatology, Emory University School of Medicine, Atlanta, Georgia 30322, USA
    J Med Chem 49:3426-7. 2006
    ..A separation of honokiol 1 from the closely structurally related magnolol 2 was developed. Honokiol demonstrated weak activity against HIV-1 in human lymphocytes...
  60. pmc Synthesis, cytotoxicity, and antiviral activities of new neolignans related to honokiol and magnolol
    Franck Amblard
    Department of Pediatrics and Dermatology, Emory University School of Medicine, Atlanta, GA 30322, USA
    Bioorg Med Chem Lett 17:4428-31. 2007
    ..Certain compounds exhibited specific anti-proliferation activity against SVR cells and moderate anti-HIV-1 activity in primary human lymphocytes. Compound 5h was the most potent compound and its anti-tumor activity was evaluated in vivo...
  61. pmc Synthesis and evaluation of 3'-azido-2',3'-dideoxypurine nucleosides as inhibitors of human immunodeficiency virus
    Hong Wang Zhang
    Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Veterans Affairs Medical Center, Atlanta, GA 30033, USA
    Bioorg Med Chem Lett 20:60-4. 2010
    ..Among the synthesized compounds, several show potent and selective anti-HIV activity in primary lymphocytes...
  62. pmc Prevention of rectal SHIV transmission in macaques by daily or intermittent prophylaxis with emtricitabine and tenofovir
    J Gerardo Garcia-Lerma
    Division of HIV AIDS Prevention, National Center for HIV AIDS, Viral Hepatitis, STD, and TB Prevention, Centers for Disease Control and Prevention, Atlanta, Georgia, USA
    PLoS Med 5:e28. 2008
    ..We evaluated daily and intermittent PrEP regimens of increasing antiviral activity in a macaque model that closely resembles human transmission...
  63. ncbi request reprint The boron-neutron capture agent beta-D-5-o-carboranyl-2'-deoxyuridine accumulates preferentially in dividing brain tumor cells
    Casey Moore
    Department of Nuclear Engineering, Georgia Institute of Technology, Atlanta, GA, USA
    J Neurooncol 74:275-80. 2005
    ..Therefore, dosimetry calculations that include the spatial distribution of cycling cells may be warranted for D-CDU...
  64. pmc Antiretroviral therapy in macrophages: implication for HIV eradication
    Christina Gavegnano
    Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA, USA
    Antivir Chem Chemother 20:63-78. 2009
    ....
  65. ncbi request reprint 5-(Phenylthio)acyclouridine: a powerful enhancer of oral uridine bioavailability: relevance to chemotherapy with 5-fluorouracil and other uridine rescue regimens
    Omar N Al Safarjalani
    Department of Pharmacology and Toxicology, Comprehensive Cancer Center, Center for AIDS Research, University of Alabama at Birmingham, Birmingham, AL 35294, USA
    Cancer Chemother Pharmacol 55:541-51. 2005
    ..PTAU is fully absorbed after oral administration with 100% oral bioavailability...
  66. ncbi request reprint Retrovirus reverse transcriptases containing a modified YXDD motif
    Prem L Sharma
    Laboratory of Biochemical Pharmacology and Department of Pediatrics, Emory University School of Medicine, Atlanta, GA, USA
    Antivir Chem Chemother 16:169-82. 2005
    ....
  67. ncbi request reprint Viral pharmacodynamic model for (-)-beta-2',3'-dideoxy-5-fluoro-3'-thiacytidine (emtricitabine) in chronically infected woodchucks
    Selwyn J Hurwitz
    Department of Pediatrics, Emory University School of Medicine, Veterans Affairs Medical Center, Decatur, GA, USA
    Antivir Chem Chemother 13:165-76. 2002
    ....
  68. ncbi request reprint The synthesis and biological evaluation of novel bridging nucleoside analogues
    Cecilia H Marzabadi
    Department of Chemistry, Hunter College CUNY, 695 Park Avenue, New York, NY 10021, USA
    Bioorg Med Chem 10:273-81. 2002
    ..One compound displayed anti-herpes simplex virus type-1 activity in Vero cells. Cytotoxicity measurements were also obtained...
  69. ncbi request reprint New manzamine alkaloids with activity against infectious and tropical parasitic diseases from an Indonesian sponge
    Karumanchi V Rao
    The Department of Pharmacognosy and National Center for Natural Products Research, School of Pharmacy, The University of Mississippi, University, MS 38677, USA
    J Nat Prod 66:823-8. 2003
    ..The bioactivity and SAR of the manzamines against malaria, TB, and leishmania are also presented. The structural revision of two previously reported pyrazoles as uracil and thymine is also discussed...
  70. ncbi request reprint l-2',3'-Didehydro-2',3'-dideoxy-3'-fluoronucleosides: synthesis, anti-HIV activity, chemical and enzymatic stability, and mechanism of resistance
    Youhoon Chong
    Department of Pharmaceutical and Biomedical Sciences, College of Pharmacy, The University of Georgia, Athens, Georgia 30602, USA
    J Med Chem 46:3245-56. 2003
    ..The biological results suggest that, in addition to the sugar conformation, the base moiety may also play a role in their interaction with the M184V RT...
  71. ncbi request reprint Probing the molecular mechanisms of AZT drug resistance mediated by HIV-1 reverse transcriptase using a transient kinetic analysis
    Adrian S Ray
    Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, Connecticut 06520, USA
    Biochemistry 42:8831-41. 2003
    ..Structure-activity studies of chain terminator removal suggest that analogues that form tight interactions with residues in the RT active site may be more prone to resistance mechanisms mediated by removal...
  72. ncbi request reprint Probing the mechanistic consequences of 5-fluorine substitution on cytidine nucleotide analogue incorporation by HIV-1 reverse transcriptase
    Adrian S Ray
    Department of Pharmacology, Yale University School of Medicine, New Haven, Conn, USA
    Antivir Chem Chemother 14:115-25. 2003
    ....
  73. ncbi request reprint Assessment of the relative potency of emtricitabine and lamivudine
    Raymond F Schinazi
    J Acquir Immune Defic Syndr 34:243-5; author reply 245-6. 2003
  74. ncbi request reprint Acyclovir is activated into a HIV-1 reverse transcriptase inhibitor in herpesvirus-infected human tissues
    Andrea Lisco
    Eunice Kennedy Shriver National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, MD 20892, USA
    Cell Host Microbe 4:260-70. 2008
    ..These data suggest that ACV anti-HIV-1 activity may contribute to the response of HIV/HHV-coinfected patients to ACV treatment and could guide strategies for the development of new HIV-1 RT inhibitors...
  75. ncbi request reprint HIV-1 resistance profile of the novel nucleoside reverse transcriptase inhibitor beta-D-2',3'-dideoxy-2',3'-didehydro-5-fluorocytidine (Reverset)
    Romas Geleziunas
    Department of Virology, The DuPont Pharmaceuticals Company Bristol Myers Squibb Pharmaceuticals Company, Del, USA
    Antivir Chem Chemother 14:49-59. 2003
    ..3- to 8.7-fold resistance to D-d4FC in vitro. These findings suggest that D-d4FC may represent an alternative NRTI for the treatment of individuals infected with lamivudine- and zidovudine-resistant strains of HIV-1...
  76. ncbi request reprint Cellular pharmacology of D-d4FC, a nucleoside analogue active against drug-resistant HIV
    Susan Erickson-Viitanen
    DuPont Pharmaceuticals Co Bristol Myers Squibb Pharmaceuticals Co, Wilmington, Del, USA
    Antivir Chem Chemother 14:39-47. 2003
    ....
  77. ncbi request reprint Synthesis of oxathiolane imidazole nucleosides
    Ayse Kocabalkanli
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Istanbul, 34452 Beyazit Istanbul, Turkey
    Farmaco 57:993-7. 2002
    ..Res. 1-11 (1994) 25) in human peripheral blood mononuclear (PBM) cells, the synthesized nucleosides did not show significant activity up to 100 microM against HIV-1...
  78. ncbi request reprint Synthesis and potent anti-HIV activity of L-2',3'-didehydro-2',3'-dideoxy-2'-fluoro-4'-thiocytidine
    Yongseok Choi
    Department of Pharmaceutical and Biomedical Sciences, College of Pharmacy, The University of Georgia, Athens, Georgia 30602, USA
    Org Lett 4:305-7. 2002
    ..The synthesized compound 11 shows potent antiviral activity against HIV-1...
  79. ncbi request reprint Structure-activity relationships of 2'-fluoro-2',3'-unsaturated D-nucleosides as anti-HIV-1 agents
    Kyeong Lee
    Department of Pharmaceutical and Biomedical Sciences, College of Pharmacy, rdag, Athens, Georgia 30602, USA
    J Med Chem 45:1313-20. 2002
    ..The implications for drug resistance of the titled nucleosides with respect to lamivudine-resistant variants (M184V) were also examined, and no significant cross-resistance with the variants was observed with the D-series...
  80. ncbi request reprint Insights into the molecular mechanism of inhibition and drug resistance for HIV-1 RT with carbovir triphosphate
    Adrian S Ray
    Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, Connecticut 06520 8066, USA
    Biochemistry 41:5150-62. 2002
    ..This compound shows promise as a potent antiviral especially with the drug resistant M184V HIV-1 RT that is so often encountered in a clinical setting...
  81. pmc Virulence and reduced fitness of simian immunodeficiency virus with the M184V mutation in reverse transcriptase
    Koen K A Van Rompay
    California Regional Primate Research Center, University of California, Davis, California 95616, USA
    J Virol 76:6083-92. 2002
    ..These data demonstrate that the M184V mutation in SIV conferred a slightly reduced fitness but did not affect disease outcome...
  82. ncbi request reprint Molecular mechanism of DApd/DXG against zidovudine- and lamivudine- drug resistant mutants: a molecular modelling approach
    Youhoon Chong
    Department of Pharmaceutical and Biomedical Sciences, College of Pharmacy, The University of Georgia, Athens, USA
    Antivir Chem Chemother 13:115-28. 2002
    ..The enzyme-inhibitor complexes with good binding affinity showed tight binding modes by closing the gap between the two domains, whereas weak inhibitors gave open and loose complexes...
  83. ncbi request reprint Stereoselective synthesis and antiviral activity of D-2',3'-didehydro-2',3'-dideoxy-2'-fluoro-4'-thionucleosides
    Youhoon Chong
    Department of Pharmaceutical and Biomedical Sciences, College of Pharmacy, The University of Georgia, Athens, Georgia 30602, USA
    J Med Chem 45:4888-98. 2002
    ....
  84. ncbi request reprint Interactions of enantiomers of 2',3'-didehydro-2',3'-dideoxy-fluorocytidine with wild type and M184V mutant HIV-1 reverse transcriptase
    Adrian S Ray
    Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06520 8066, USA
    Antiviral Res 56:189-205. 2002
    ....
  85. ncbi request reprint Synthesis, anti-HIV activity, and molecular mechanism of drug resistance of L-2',3'-didehydro-2',3'-dideoxy-2'-fluoro-4'-thionucleosides
    Hyunah Choo
    Department of Pharmaceutical and Biomedical Sciences, College of Pharmacy, The University of Georgia, Athens, Georgia 30602, USA
    J Med Chem 46:389-98. 2003
    ....
  86. ncbi request reprint 2'-Fluoro-4'-thio-2',3'-unsaturated nucleosides: anti-HIV activity, resistance profile, and molecular modeling studies
    Youhoon Chong
    Department of Pharmaceutical and Biomedical Sciences, College of Pharmacy, The University of Georgia, Athens, Georgia 30602, USA
    Nucleosides Nucleotides Nucleic Acids 22:611-5. 2003
    ..Molecular modeling studies revealed that the unnatural sugar moiety of the L-nucleosides as well as 4'-sulfur atom of the D-isomer has a steric conflict with the bulky side chain of valine 184, resulting in cross-resistance...
  87. ncbi request reprint Investigating the effects of stereochemistry on incorporation and removal of 5-fluorocytidine analogs by mitochondrial DNA polymerase gamma: comparison of D- and L-D4FC-TP
    Eisuke Murakami
    Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06520 8066, USA
    Antiviral Res 62:57-64. 2004
    ....
  88. ncbi request reprint Enantioselective synthesis and antiviral activity of purine and pyrimidine cyclopentenyl C-nucleosides
    Jagadeeshwar R Rao
    The University of Georgia College of Pharmacy, Athens, GA 30602, USA
    Bioorg Med Chem 15:839-46. 2007
    ..Synthesized compounds were evaluated as potential antiviral agents against HIV, SARSCoV, Punta Toro, West Nile, and Cowpox viruses. However, only 9-deazaneplanocin A (1) exhibited moderate anti-HIV activity...
  89. ncbi request reprint Anti-HIV activity of (-)-(2R,4R)-1- (2-hydroxymethyl-1,3-dioxolan-4-yl)-thymine against drug-resistant HIV-1 mutants and studies of its molecular mechanism
    Chung K Chu
    College of Pharmacy, The University of Georgia, Athens, 30602, USA
    J Med Chem 48:3949-52. 2005
    ..The key reason for this interesting antiviral activity profile is the presence of a dioxolane ring...
  90. ncbi request reprint The 3'-azido group is not the primary determinant of 3'-azido-3'-deoxythymidine (AZT) responsible for the excision phenotype of AZT-resistant HIV-1
    Nicolas Sluis-Cremer
    University of Pittsburgh School of Medicine, Division of Infectious Diseases, Pittsburgh, PA 15261, USA
    J Biol Chem 280:29047-52. 2005
    ..Other structural components, such as the base, must play a role in defining the specificity of the excision phenotype arising from AZT resistance mutations...
  91. pmc Synthesis and anti-HIV activity of D- and L-thietanose nucleosides
    Hyunah Choo
    College of Pharmacy, The University of Georgia, Athens, Georgia 30602, USA
    J Med Chem 49:1635-47. 2006
    ....
  92. ncbi request reprint Synthesis and anti-HIV activity of beta-D-3'-azido-2',3'-unsaturated nucleosides and beta-D-3'-azido-3'-deoxyribofuranosylnucleosides
    Srinivas Gadthula
    Department of Pharmaceutical and Biomedical Sciences, College of Pharmacy, The University of Georgia, Athens, Georgia 30602, USA
    Nucleosides Nucleotides Nucleic Acids 24:1707-27. 2005
    ..The resultant protected nucleosides were converted to target nucleosides using appropriate chemical modifications. The final nucleosides were evaluated as potential anti-HIV agents...
  93. ncbi request reprint Phosphoramidate and phosphate prodrugs of (-)-beta-D-(2R,4R)-dioxolane-thymine: synthesis, anti-HIV activity and stability studies
    Yuzeng Liang
    The University of Georgia, College of Pharmacy, Athens, GA 30602, USA
    Bioorg Med Chem 14:2178-89. 2006
    ..Long-chain lipid phosphates, although showed potent anti-HIV activity, exhibited increased cytotoxicity...
  94. ncbi request reprint Synthesis of 5-haloethynyl- and 5-(1,2-dihalo)vinyluracil nucleosides: antiviral activity and cellular toxicity
    Vanessa Escuret
    Institut de Chimie Organique et Analytique, ICOA UMR 6005, UFR Sciences, BP 6759, 45067 Orleans Cedex 2, France
    Bioorg Med Chem 13:6015-24. 2005
    ..2) and the 5-(1-chloro-2-iodo)vinyluridine (SI > 2.8)...
  95. pmc Quantifying mixed populations of drug-resistant human immunodeficiency virus type 1
    Michael J Moser
    Eragen Biosciences, Inc, 918 Deming Way, Madison, WI 53717, USA
    Antimicrob Agents Chemother 49:3334-40. 2005
    ..MultiCode-RTx could be applied to other drug-selected mutations in the viral genome or for applications where single-base changes in DNA or RNA occur at frequencies reaching 0.01% to 1%, respectively...
  96. ncbi request reprint Synthesis and biological evaluation of novel 5(H)-phenanthridin-6-ones, 5(H)-phenanthridin-6-one diketo acid, and polycyclic aromatic diketo acid analogs as new HIV-1 integrase inhibitors
    Shivaputra Patil
    Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, TN 38163, USA
    Bioorg Med Chem 15:1212-28. 2007
    ....
  97. pmc D- and L-2',3'-didehydro-2',3'-dideoxy-3'-fluoro-carbocyclic nucleosides: synthesis, anti-HIV activity and mechanism of resistance
    Jianing Wang
    College of Pharmacy, The University of Georgia, Athens, Georgia 30602, USA
    J Med Chem 50:1828-39. 2007
    ....
  98. ncbi request reprint Synthesis, antiviral activity, and mechanism of drug resistance of D- and L-2',3'-didehydro-2',3'-dideoxy-2'-fluorocarbocyclic nucleosides
    Jianing Wang
    College of Pharmacy, The University of Georgia, Athens, Georgia 30602, USA
    J Med Chem 48:3736-48. 2005
    ..The significant difference of antiviral activity between carbovir and its analogue L-2'F-C-d4G 25 may be due to distortion of the phenyl ring of Tyr115 in the L-2'F-C-d4G-TP/HIV-RT complex, which resulted in a poor pi-pi interaction...
  99. ncbi request reprint Synthesis, structure-activity relationships, and mechanism of drug resistance of D- and L-beta-3'-fluoro-2',3'-unsaturated-4'-thionucleosides as anti-HIV agents
    Wei Zhu
    Department of Pharmaceutical and Biomedical Sciences, College of Pharmacy, The University of Georgia, Athens, Georgia 30602, USA
    J Med Chem 47:1631-40. 2004
    ..Like other unnatural L-nucleosides, the unfavorable steric hindrance of the sugar moiety of L-3'F-4'Sd4CTP with the side chain of Val184 explains its significant cross-resistance to the M184V mutant...
  100. pmc Relationship between antiviral activity and host toxicity: comparison of the incorporation efficiencies of 2',3'-dideoxy-5-fluoro-3'-thiacytidine-triphosphate analogs by human immunodeficiency virus type 1 reverse transcriptase and human mitochondrial DNA
    Joy Y Feng
    Gilead Sciences, Durham, North Carolina 27707, USA
    Antimicrob Agents Chemother 48:1300-6. 2004
    ..6-fold slower than the excision of dCMP. These results demonstrate that there are clear differences between HIV-1 RT and polymerase gamma in terms of preferences for substrate structure...

Research Grants5

  1. HIV DART:Frontiers in Drug Development for ARV Therapies
    RAYMOND SCHINAZI; Fiscal Year: 2007
    ..Support is requested to help defray the publications costs of the abstract book and for equipment used to facilitate delivery and display of the oral and poster presentations. ..
  2. NUCLEOSIDES WITH DUAL ANTI-HIV AND HBV ACTIVITY
    RAYMOND SCHINAZI; Fiscal Year: 2007
    ..abstract_text> ..