Yaya Liu

Summary

Affiliation: Abbott Laboratories
Country: USA

Publications

  1. doi Identification of aryl dihydrouracil derivatives as palm initiation site inhibitors of HCV NS5B polymerase
    Yaya Liu
    Antiviral Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 22:3747-50. 2012
  2. ncbi Use of a fluorescence plate reader for measuring kinetic parameters with inner filter effect correction
    Y Liu
    Antiviral Department, Infectious Disease Research, Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, Illinois, 60064 3500, USA
    Anal Biochem 267:331-5. 1999
  3. ncbi Investigating the origin of the slow-binding inhibition of HCV NS3 serine protease by a novel substrate based inhibitor
    Yaya Liu
    Antiviral Department, Infectious Disease Research and Advanced Technology, Pharmaceutical Discovery, Abbott Laboratories, Abbott Park, Illinois 60064 6217, USA
    Biochemistry 42:8862-9. 2003
  4. ncbi Hepatitis C NS3 protease inhibition by peptidyl-alpha-ketoamide inhibitors: kinetic mechanism and structure
    Yaya Liu
    Antiviral Research, Infectious Disease Research and Advanced Technology, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064 6217, USA
    Arch Biochem Biophys 421:207-16. 2004
  5. doi Identification of halosalicylamide derivatives as a novel class of allosteric inhibitors of HCV NS5B polymerase
    Yaya Liu
    Antiviral Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 18:3173-7. 2008
  6. ncbi A fluorescence polarization-based assay for peptidyl prolyl cis/trans isomerase cyclophilin A
    Yaya Liu
    Antiviral Research R4CQ AP52, Infectious Disease Research, Abbott Laboratories, Abbott Park, IL 60064, USA
    Anal Biochem 356:100-7. 2006
  7. ncbi Mechanistic study of HCV polymerase inhibitors at individual steps of the polymerization reaction
    Yaya Liu
    Antiviral Research, Infectious Disease Research, Abbott Laboratories, Abbott Park, Illinois 60064 6217, USA
    Biochemistry 45:11312-23. 2006
  8. doi Hepatitis C NS5B polymerase inhibitors: functional equivalents for the benzothiadiazine moiety
    Douglas K Hutchinson
    Department of Antiviral Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 21:1876-9. 2011
  9. doi Aryl uracil inhibitors of hepatitis C virus NS5B polymerase: synthesis and characterization of analogs with a fused 5,6-bicyclic ring motif
    A Chris Krueger
    AbbVie Inc, 1 North Waukegan Road, North Chicago, IL 60064, USA
    Bioorg Med Chem Lett 23:3487-90. 2013
  10. ncbi Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of unsymmetrical 1-hydroxy-4,4-dialkyl-3-oxo-3,4-dihydronaphthalene benzothiadiazine derivatives
    A Chris Krueger
    Infectious Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 17:2289-92. 2007

Detail Information

Publications22

  1. doi Identification of aryl dihydrouracil derivatives as palm initiation site inhibitors of HCV NS5B polymerase
    Yaya Liu
    Antiviral Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 22:3747-50. 2012
    ..Therefore, aryl dihydrouracil derivatives represent a novel class of palm initiation site inhibitors of HCV NS5B polymerase...
  2. ncbi Use of a fluorescence plate reader for measuring kinetic parameters with inner filter effect correction
    Y Liu
    Antiviral Department, Infectious Disease Research, Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, Illinois, 60064 3500, USA
    Anal Biochem 267:331-5. 1999
    ..We demonstrate that the inner filter effect correction of microtiter plate reader velocities enables rapid measurement of Ki and Ki' values and kinetic inhibition mechanisms for HCV NS3 protease inhibitors...
  3. ncbi Investigating the origin of the slow-binding inhibition of HCV NS3 serine protease by a novel substrate based inhibitor
    Yaya Liu
    Antiviral Department, Infectious Disease Research and Advanced Technology, Pharmaceutical Discovery, Abbott Laboratories, Abbott Park, Illinois 60064 6217, USA
    Biochemistry 42:8862-9. 2003
    ..The mechanism of inhibition for this S-S linked substrate based inhibitor is likely due to oxidation of cysteines involved in chelation of the structural zinc atom...
  4. ncbi Hepatitis C NS3 protease inhibition by peptidyl-alpha-ketoamide inhibitors: kinetic mechanism and structure
    Yaya Liu
    Antiviral Research, Infectious Disease Research and Advanced Technology, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064 6217, USA
    Arch Biochem Biophys 421:207-16. 2004
    ..These results are quite different from peptidyl-alpha-ketoacid inhibition of HCV protease, which reportedly undergoes no notable conformational changes and proceeds with a two-step slow-binding kinetic mechanism...
  5. doi Identification of halosalicylamide derivatives as a novel class of allosteric inhibitors of HCV NS5B polymerase
    Yaya Liu
    Antiviral Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 18:3173-7. 2008
    ..Therefore, halosalicylamides represent a novel class of allosteric inhibitors of HCV NS5B polymerase...
  6. ncbi A fluorescence polarization-based assay for peptidyl prolyl cis/trans isomerase cyclophilin A
    Yaya Liu
    Antiviral Research R4CQ AP52, Infectious Disease Research, Abbott Laboratories, Abbott Park, IL 60064, USA
    Anal Biochem 356:100-7. 2006
    ....
  7. ncbi Mechanistic study of HCV polymerase inhibitors at individual steps of the polymerization reaction
    Yaya Liu
    Antiviral Research, Infectious Disease Research, Abbott Laboratories, Abbott Park, Illinois 60064 6217, USA
    Biochemistry 45:11312-23. 2006
    ..This information will be very important in designing combination therapies using two small molecule drugs to treat hepatitis C virus...
  8. doi Hepatitis C NS5B polymerase inhibitors: functional equivalents for the benzothiadiazine moiety
    Douglas K Hutchinson
    Department of Antiviral Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 21:1876-9. 2011
    ..Several of these compounds exhibited potent activity in enzymatic and replicon assays...
  9. doi Aryl uracil inhibitors of hepatitis C virus NS5B polymerase: synthesis and characterization of analogs with a fused 5,6-bicyclic ring motif
    A Chris Krueger
    AbbVie Inc, 1 North Waukegan Road, North Chicago, IL 60064, USA
    Bioorg Med Chem Lett 23:3487-90. 2013
    ..Several analogs display replicon cell culture potencies in the low nanomolar range along with excellent rat pharmacokinetic values...
  10. ncbi Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of unsymmetrical 1-hydroxy-4,4-dialkyl-3-oxo-3,4-dihydronaphthalene benzothiadiazine derivatives
    A Chris Krueger
    Infectious Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 17:2289-92. 2007
    ..Structure-activity relationship patterns for this class of compounds are discussed. It was found that the saturated alkane dialkyl units provided the most active analogs...
  11. doi Des-A-ring benzothiadiazines: inhibitors of HCV genotype 1 NS5B RNA-dependent RNA polymerase
    Pamela L Donner
    Antiviral Research, Global Pharmaceutical Research, and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 18:2735-8. 2008
    ..We observed that small aromatic rings and alkenyl groups appended to the 5-position of the B-ring were optimal, resulting in inhibitors with low nanomolar potencies...
  12. doi Hepatitis C NS5B polymerase inhibitors: 4,4-Dialkyl-1-hydroxy-3-oxo-3,4-dihydronaphthalene-3-yl benzothiadiazine derivatives
    Douglas K Hutchinson
    Department of Antiviral Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 18:3887-90. 2008
    ..A number of these compounds exhibited potent activity against genotypes 1a and 1b HCV polymerase in both enzymatic and cell culture activities. A representative compound also showed favorable pharmacokinetics in the rat...
  13. ncbi Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-alkyl-4-hydroxyquinolon-3-yl-benzothiadiazine sulfamides
    A Chris Krueger
    Infectious Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 16:3367-70. 2006
    ..Substituted N-alkyl-4-hydroxyquinolon-3-yl-benzothiadiazine sulfamides were investigated as inhibitors of genotype 1 HCV polymerase. Structure-activity relationship patterns for this class of compounds are discussed...
  14. doi Synthesis and biological characterization of B-ring amino analogues of potent benzothiadiazine hepatitis C virus polymerase inhibitors
    John T Randolph
    Global Pharmaceutical Research and Development, Abbott, 200 Abbott Park Road, Abbott Park, Illinois 60064 6217, USA
    J Med Chem 52:3174-83. 2009
    ..Compound 30 is a potent inhibitor in replicon assays, with EC(50) values of 10 and 6 nM against genotypes 1a and 1b, respectively...
  15. ncbi Synthesis and SAR of novel 1,1-dialkyl-2(1H)-naphthalenones as potent HCV polymerase inhibitors
    Todd D Bosse
    Infectious Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 18:568-70. 2008
    ..This investigation led to the discovery of potent inhibitors of the hepatitis C virus at low nanomolar concentrations in both enzymatic and cell-based HCV genotype 1a assays...
  16. ncbi Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-1-heteroalkyl-4-hydroxyquinolon-3-yl-benzothiadiazines
    John K Pratt
    Infectious Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 15:1577-82. 2005
    ..The most potent inhibitors contained small alkyl or carbocyclic substituents and exhibited IC50's of 50-100 and 200-400 nM against genotype 1b and 1a HCV polymerase, respectively...
  17. doi Inhibitors of hepatitis C virus polymerase: synthesis and biological characterization of unsymmetrical dialkyl-hydroxynaphthalenoyl-benzothiadiazines
    Rolf Wagner
    Global Pharmaceutical Research and Development, Abbott, Abbott Park, Illinois 60064, USA
    J Med Chem 52:1659-69. 2009
    ..It also displayed an excellent pharmacokinetic profile in rats, with a plasma elimination half-life after intravenous dosing of 4.5 h, oral bioavailability of 77%, and a peak liver concentration of 21.8 microg/mL...
  18. doi Methods to measure the intracellular concentration of unlabeled compounds within cultured cells using liquid chromatography/tandem mass spectrometry
    Lynn M Colletti
    Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Anal Biochem 383:186-93. 2008
    ..This assay was used to understand differences in cellular potency between compounds and the effects of serum proteins on the metabolic stability of compounds during incubation with cells...
  19. doi Water-soluble prodrugs of the human immunodeficiency virus protease inhibitors lopinavir and ritonavir
    David A DeGoey
    Antiviral Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA
    J Med Chem 52:2964-70. 2009
    ..A direct synthetic process for the preparation of OMP and OEP prodrugs was developed, and the improved synthetic method may be applicable to the preparation of analogous soluble prodrugs of other drug classes with limited solubility...
  20. pmc Selection and characterization of varicella-zoster virus variants resistant to (R)-9-[4-hydroxy-2-(hydroxymethy)butyl]guanine
    T I Ng
    Department of Anti Infective Research, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, Illinois 60064, USA
    Antimicrob Agents Chemother 45:1629-36. 2001
    ..All of these changes introduced frameshift mutations in the TK gene resulting in the expression of truncated polypeptides. H2G-resistant viruses were cross-resistant to ACV, and vice versa...
  21. doi Cracking the molecular weight barrier: fragment screening of an aminotransferase using an NMR-based functional assay
    Renaldo Mendoza
    Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, United States
    Bioorg Med Chem Lett 21:5248-50. 2011
    ..Several fragments which inhibit BCATc were discovered using this assay and these may serve as novel cores for the development of potent BCATc inhibitors...
  22. ncbi ALARM NMR: a rapid and robust experimental method to detect reactive false positives in biochemical screens
    Jeffrey R Huth
    Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064, USA
    J Am Chem Soc 127:217-24. 2005
    ..In addition, a new filtering tool has been developed on the basis of the ALARM NMR data that can augment current in silico programs for identifying nuisance compounds and improving the process of hit triage...