Research Topics
| Yaya LiuSummaryAffiliation: Abbott Laboratories Country: USA Publications
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Detail Information
Publications
Identification of aryl dihydrouracil derivatives as palm initiation site inhibitors of HCV NS5B polymeraseYaya 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...- Identification of halosalicylamide derivatives as a novel class of allosteric inhibitors of HCV NS5B polymeraseYaya 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... 
Use of a fluorescence plate reader for measuring kinetic parameters with inner filter effect correctionY 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...- Mechanistic study of HCV polymerase inhibitors at individual steps of the polymerization reactionYaya 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... - A fluorescence polarization-based assay for peptidyl prolyl cis/trans isomerase cyclophilin AYaya Liu
Antiviral Research R4CQ AP52, Infectious Disease Research, Abbott Laboratories, Abbott Park, IL 60064, USA
Anal Biochem 356:100-7. 2006.... - Hepatitis C NS3 protease inhibition by peptidyl-alpha-ketoamide inhibitors: kinetic mechanism and structureYaya 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... - Investigating the origin of the slow-binding inhibition of HCV NS3 serine protease by a novel substrate based inhibitorYaya 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... - Hepatitis C NS5B polymerase inhibitors: functional equivalents for the benzothiadiazine moietyDouglas 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... - Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of unsymmetrical 1-hydroxy-4,4-dialkyl-3-oxo-3,4-dihydronaphthalene benzothiadiazine derivativesA 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... - Des-A-ring benzothiadiazines: inhibitors of HCV genotype 1 NS5B RNA-dependent RNA polymerasePamela 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... - Hepatitis C NS5B polymerase inhibitors: 4,4-Dialkyl-1-hydroxy-3-oxo-3,4-dihydronaphthalene-3-yl benzothiadiazine derivativesDouglas 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... - Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-alkyl-4-hydroxyquinolon-3-yl-benzothiadiazine sulfamidesA 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... - Synthesis and biological characterization of B-ring amino analogues of potent benzothiadiazine hepatitis C virus polymerase inhibitorsJohn 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... - Synthesis and SAR of novel 1,1-dialkyl-2(1H)-naphthalenones as potent HCV polymerase inhibitorsTodd 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... - Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-1-heteroalkyl-4-hydroxyquinolon-3-yl-benzothiadiazinesJohn 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... - Inhibitors of hepatitis C virus polymerase: synthesis and biological characterization of unsymmetrical dialkyl-hydroxynaphthalenoyl-benzothiadiazinesRolf 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... - Methods to measure the intracellular concentration of unlabeled compounds within cultured cells using liquid chromatography/tandem mass spectrometryLynn 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... - Water-soluble prodrugs of the human immunodeficiency virus protease inhibitors lopinavir and ritonavirDavid 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... 
Selection and characterization of varicella-zoster virus variants resistant to (R)-9-[4-hydroxy-2-(hydroxymethy)butyl]guanineT 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...- Cracking the molecular weight barrier: fragment screening of an aminotransferase using an NMR-based functional assayRenaldo 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... - ALARM NMR: a rapid and robust experimental method to detect reactive false positives in biochemical screensJeffrey 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...