Angela M Lam

Summary

Affiliation: Pharmasset Inc
Country: USA

Publications

  1. pmc PSI-7851, a pronucleotide of beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine monophosphate, is a potent and pan-genotype inhibitor of hepatitis C virus replication
    Angela M Lam
    Pharmasset, Inc, 303A College Road East, Princeton, NJ 08540, USA
    Antimicrob Agents Chemother 54:3187-96. 2010
  2. pmc Hepatitis C virus nucleotide inhibitors PSI-352938 and PSI-353661 exhibit a novel mechanism of resistance requiring multiple mutations within replicon RNA
    Angela M Lam
    Pharmasset, Inc, 303A College Road East, Princeton, NJ 08540, USA
    J Virol 85:12334-42. 2011
  3. pmc Inhibition of hepatitis C virus replicon RNA synthesis by PSI-352938, a cyclic phosphate prodrug of β-D-2'-deoxy-2'-α-fluoro-2'-β-C-methylguanosine
    Angela M Lam
    Pharmasset, Inc, 303A College Road East, Princeton, NJ 08540, USA
    Antimicrob Agents Chemother 55:2566-75. 2011
  4. ncbi β-D-2'-α-F-2'-β-C-Methyl-6-O-substituted 3',5'-cyclic phosphate nucleotide prodrugs as inhibitors of hepatitis C virus replication: a structure-activity relationship study
    Jinfa Du
    Pharmasset, Inc, Princeton 303A College Road East, Princeton, NJ 08540, USA
    Bioorg Med Chem Lett 22:5924-9. 2012
  5. doi Discovery of a β-d-2'-deoxy-2'-α-fluoro-2'-β-C-methyluridine nucleotide prodrug (PSI-7977) for the treatment of hepatitis C virus
    Michael J Sofia
    Pharmasset, Inc, 303A College Road East, Princeton, New Jersey 08540, USA
    J Med Chem 53:7202-18. 2010
  6. pmc Activity and the metabolic activation pathway of the potent and selective hepatitis C virus pronucleotide inhibitor PSI-353661
    Phillip A Furman
    Pharmasset, Inc, Princeton, NJ 08540, USA
    Antiviral Res 91:120-32. 2011
  7. pmc Genotype and subtype profiling of PSI-7977 as a nucleotide inhibitor of hepatitis C virus
    Angela M Lam
    Pharmasset, Inc, Princeton, New Jersey, USA
    Antimicrob Agents Chemother 56:3359-68. 2012
  8. pmc Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977
    Eisuke Murakami
    Pharmasset, Inc, Princeton, New Jersey 08540, USA
    J Biol Chem 285:34337-47. 2010
  9. ncbi Use of 2'-spirocyclic ethers in HCV nucleoside design
    Jinfa Du
    Pharmasset, Inc, 303A College Road East, Princeton, New Jersey 08540, United States
    J Med Chem 57:1826-35. 2014
  10. pmc Metabolic activation of the anti-hepatitis C virus nucleotide prodrug PSI-352938
    Congrong Niu
    Pharmasset, Inc, Princeton, New Jersey, USA
    Antimicrob Agents Chemother 56:3767-75. 2012

Collaborators

Detail Information

Publications15

  1. pmc PSI-7851, a pronucleotide of beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine monophosphate, is a potent and pan-genotype inhibitor of hepatitis C virus replication
    Angela M Lam
    Pharmasset, Inc, 303A College Road East, Princeton, NJ 08540, USA
    Antimicrob Agents Chemother 54:3187-96. 2010
    ..Clearance studies using replicon cells demonstrated that PSI-7851 was able to clear cells of HCV replicon RNA and prevent viral rebound...
  2. pmc Hepatitis C virus nucleotide inhibitors PSI-352938 and PSI-353661 exhibit a novel mechanism of resistance requiring multiple mutations within replicon RNA
    Angela M Lam
    Pharmasset, Inc, 303A College Road East, Princeton, NJ 08540, USA
    J Virol 85:12334-42. 2011
    ....
  3. pmc Inhibition of hepatitis C virus replicon RNA synthesis by PSI-352938, a cyclic phosphate prodrug of β-D-2'-deoxy-2'-α-fluoro-2'-β-C-methylguanosine
    Angela M Lam
    Pharmasset, Inc, 303A College Road East, Princeton, NJ 08540, USA
    Antimicrob Agents Chemother 55:2566-75. 2011
    ..PSI-352938 is currently being evaluated in a phase I clinical study in genotype 1-infected individuals...
  4. ncbi β-D-2'-α-F-2'-β-C-Methyl-6-O-substituted 3',5'-cyclic phosphate nucleotide prodrugs as inhibitors of hepatitis C virus replication: a structure-activity relationship study
    Jinfa Du
    Pharmasset, Inc, Princeton 303A College Road East, Princeton, NJ 08540, USA
    Bioorg Med Chem Lett 22:5924-9. 2012
    ..Compounds 12, 13 and 19 also demonstrated the ability to effectively deliver in vivo high levels of active nucleoside phosphates to rat liver...
  5. doi Discovery of a β-d-2'-deoxy-2'-α-fluoro-2'-β-C-methyluridine nucleotide prodrug (PSI-7977) for the treatment of hepatitis C virus
    Michael J Sofia
    Pharmasset, Inc, 303A College Road East, Princeton, New Jersey 08540, USA
    J Med Chem 53:7202-18. 2010
    ..51 (PSI-7977) was selected as a clinical development candidate...
  6. pmc Activity and the metabolic activation pathway of the potent and selective hepatitis C virus pronucleotide inhibitor PSI-353661
    Phillip A Furman
    Pharmasset, Inc, Princeton, NJ 08540, USA
    Antiviral Res 91:120-32. 2011
    ..PSI-352666 is equally active against wild-type NS5B and NS5B containing the S282T amino acid alteration...
  7. pmc Genotype and subtype profiling of PSI-7977 as a nucleotide inhibitor of hepatitis C virus
    Angela M Lam
    Pharmasset, Inc, Princeton, New Jersey, USA
    Antimicrob Agents Chemother 56:3359-68. 2012
    ....
  8. pmc Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977
    Eisuke Murakami
    Pharmasset, Inc, Princeton, New Jersey 08540, USA
    J Biol Chem 285:34337-47. 2010
    ..PSI-7411 is then consecutively phosphorylated to the diphosphate, PSI-7410, and to the active triphosphate metabolite, PSI-7409, by UMP-CMP kinase and nucleoside diphosphate kinase, respectively...
  9. ncbi Use of 2'-spirocyclic ethers in HCV nucleoside design
    Jinfa Du
    Pharmasset, Inc, 303A College Road East, Princeton, New Jersey 08540, United States
    J Med Chem 57:1826-35. 2014
    ....
  10. pmc Metabolic activation of the anti-hepatitis C virus nucleotide prodrug PSI-352938
    Congrong Niu
    Pharmasset, Inc, Princeton, New Jersey, USA
    Antimicrob Agents Chemother 56:3767-75. 2012
    ..Since CYP3A4 is highly expressed in the liver, the CYP3A4-dependent metabolism of PSI-352938 makes it an effective liver-targeted prodrug, in part accounting for the potent antiviral activity observed clinically...
  11. ncbi Discovery of a novel class of potent HCV NS4B inhibitors: SAR studies on piperazinone derivatives
    Ramesh Kakarla
    Pharmasset, Inc 303A College Road East, Princeton, New Jersey 08540, United States
    J Med Chem 57:2136-60. 2014
    ..However, the piperazonone class of compounds lacks GT-2 activity and, consequently, were not pursued further into development. ..
  12. doi Inhibition of hepatitis C virus NS5A by fluoro-olefin based γ-turn mimetics
    Wonsuk Chang
    Pharmasset, Inc, Princeton, NJ 08540, USA
    Bioorg Med Chem Lett 22:2938-42. 2012
    ....
  13. pmc Structure of hepatitis C virus polymerase in complex with primer-template RNA
    Ralph T Mosley
    Pharmasset Inc, Princeton, New Jersey, USA
    J Virol 86:6503-11. 2012
    ....
  14. doi Nucleoside analog inhibitors of hepatitis C viral replication: recent advances, challenges and trends
    Phillip A Furman
    Pharmasset, Inc, Princeton, NJ 08540, USA
    Future Med Chem 1:1429-52. 2009
    ..Herein, we discuss various classes of nucleoside inhibitors, with a focus on available structure-activity relationships, their mode of action and resistance profile...
  15. doi 2'-deoxy-2'-α-fluoro-2'-β-C-methyl 3',5'-cyclic phosphate nucleotide prodrug analogs as inhibitors of HCV NS5B polymerase: discovery of PSI-352938
    P Ganapati Reddy
    Pharmasset, Inc, 303A College Road East, Princeton, NJ 08540, USA
    Bioorg Med Chem Lett 20:7376-80. 2010
    ..These studies ultimately led to the selection of the clinical development candidate 24a (PSI-352938)...