Julie A Lemm

Summary

Affiliation: Bristol-Myers Squibb
Country: USA

Publications

  1. pmc Preclinical characterization of BMS-791325, an allosteric inhibitor of hepatitis C Virus NS5B polymerase
    Julie A Lemm
    Virology, Bristol Myers Squibb Research and Development, Wallingford, Connecticut, USA
    Antimicrob Agents Chemother 58:3485-95. 2014
  2. pmc Identification of hepatitis C virus NS5A inhibitors
    Julie A Lemm
    Department of Virology, Bristol Myers Squibb, Wallingford, CT 06492, USA
    J Virol 84:482-91. 2010
  3. doi request reprint Hepatitis C virus NS5A replication complex inhibitors. Part 6: Discovery of a novel and highly potent biarylimidazole chemotype with inhibitory activity toward genotypes 1a and 1b replicons
    Makonen Belema
    Departments of Discovery Chemistry, Virology, Lead Discovery and Optimization, Computer Assisted Drug Design, and Metabolism and Pharmacokinetics, Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States
    J Med Chem 57:1995-2012. 2014
  4. doi request reprint HCV NS5A replication complex inhibitors. Part 4. Optimization for genotype 1a replicon inhibitory activity
    Denis R St Laurent
    Departments of Medicinal Chemistry, Virology, and Computer Aided Drug Design, Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States
    J Med Chem 57:1976-94. 2014
  5. doi request reprint HCV NS5A replication complex inhibitors. Part 5: discovery of potent and pan-genotypic glycinamide cap derivatives
    Makonen Belema
    Department of Medicinal Chemistry, Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 23:4428-35. 2013
  6. doi request reprint HCV NS5A replication complex inhibitors. Part 3: discovery of potent analogs with distinct core topologies
    Omar D Lopez
    Department of Medicinal Chemistry, Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 23:779-84. 2013
  7. doi request reprint Discovery and development of hepatitis C virus NS5A replication complex inhibitors
    Makonen Belema
    Department of Discovery Chemistry, Department of Virology Discovery, and Department of Computer Assisted Drug Design, Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States
    J Med Chem 57:1643-72. 2014
  8. pmc Development of a cell-based high-throughput specificity screen using a hepatitis C virus-bovine viral diarrhea virus dual replicon assay
    Donald R O'Boyle
    Department of Virology, Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492 7660, USA Min
    Antimicrob Agents Chemother 49:1346-53. 2005
  9. doi request reprint Characterizations of HCV NS5A replication complex inhibitors
    Donald R O'Boyle Ii
    Bristol Myers Squibb Research and Development, Department of Virology Discovery, 5 Research Parkway, Wallingford, CT 06492, USA
    Virology 444:343-54. 2013
  10. doi request reprint Hepatitis C virus NS5A replication complex inhibitors: the discovery of daclatasvir
    Makonen Belema
    Departments of Discovery Chemistry, Discovery Chemistry Synthesis, Computer Assisted Drug Design, and Pharmaceutical Candidate Optimization, Virology, Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States
    J Med Chem 57:2013-32. 2014

Collaborators

Detail Information

Publications23

  1. pmc Preclinical characterization of BMS-791325, an allosteric inhibitor of hepatitis C Virus NS5B polymerase
    Julie A Lemm
    Virology, Bristol Myers Squibb Research and Development, Wallingford, Connecticut, USA
    Antimicrob Agents Chemother 58:3485-95. 2014
    ..These findings support the evaluation of BMS-791325 in combination regimens for the treatment of HCV. Phase 3 studies are ongoing...
  2. pmc Identification of hepatitis C virus NS5A inhibitors
    Julie A Lemm
    Department of Virology, Bristol Myers Squibb, Wallingford, CT 06492, USA
    J Virol 84:482-91. 2010
    ....
  3. doi request reprint Hepatitis C virus NS5A replication complex inhibitors. Part 6: Discovery of a novel and highly potent biarylimidazole chemotype with inhibitory activity toward genotypes 1a and 1b replicons
    Makonen Belema
    Departments of Discovery Chemistry, Virology, Lead Discovery and Optimization, Computer Assisted Drug Design, and Metabolism and Pharmacokinetics, Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States
    J Med Chem 57:1995-2012. 2014
    ..Securing potent GT-1a activity in a chemotype class lacking overt structural liabilities was a critical milestone in the effort to realize the full clinical potential of targeting the HCV NS5A protein. ..
  4. doi request reprint HCV NS5A replication complex inhibitors. Part 4. Optimization for genotype 1a replicon inhibitory activity
    Denis R St Laurent
    Departments of Medicinal Chemistry, Virology, and Computer Aided Drug Design, Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States
    J Med Chem 57:1976-94. 2014
    ..Additional structural refinements resulted in the identification of 30 as a potent, dual G-1a/1b HCV NS5A inhibitor. ..
  5. doi request reprint HCV NS5A replication complex inhibitors. Part 5: discovery of potent and pan-genotypic glycinamide cap derivatives
    Makonen Belema
    Department of Medicinal Chemistry, Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 23:4428-35. 2013
    ....
  6. doi request reprint HCV NS5A replication complex inhibitors. Part 3: discovery of potent analogs with distinct core topologies
    Omar D Lopez
    Department of Medicinal Chemistry, Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 23:779-84. 2013
    ....
  7. doi request reprint Discovery and development of hepatitis C virus NS5A replication complex inhibitors
    Makonen Belema
    Department of Discovery Chemistry, Department of Virology Discovery, and Department of Computer Assisted Drug Design, Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States
    J Med Chem 57:1643-72. 2014
    ..We conclude with a synopsis of the results of notable clinical trials with HCV NS5A RCIs. ..
  8. pmc Development of a cell-based high-throughput specificity screen using a hepatitis C virus-bovine viral diarrhea virus dual replicon assay
    Donald R O'Boyle
    Department of Virology, Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492 7660, USA Min
    Antimicrob Agents Chemother 49:1346-53. 2005
    ..This HCV/BVDV dual replicon assay provides a reliable format to determine the potency and specificity of HCV replicon inhibitors...
  9. doi request reprint Characterizations of HCV NS5A replication complex inhibitors
    Donald R O'Boyle Ii
    Bristol Myers Squibb Research and Development, Department of Virology Discovery, 5 Research Parkway, Wallingford, CT 06492, USA
    Virology 444:343-54. 2013
    ..The functional data supports a model of inhibition that implicates inhibitor binding by covalently combining distinct pharmacophores across an NS5A dimer interface to achieve maximal inhibition of HCV replication. ..
  10. doi request reprint Hepatitis C virus NS5A replication complex inhibitors: the discovery of daclatasvir
    Makonen Belema
    Departments of Discovery Chemistry, Discovery Chemistry Synthesis, Computer Assisted Drug Design, and Pharmaceutical Candidate Optimization, Virology, Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States
    J Med Chem 57:2013-32. 2014
    ....
  11. doi request reprint HCV NS5A replication complex inhibitors. Part 2: investigation of stilbene prolinamides
    Denis R St Laurent
    Department of Medicinal Chemistry, Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 22:6063-6. 2012
    ..These studies represent the key initial steps toward the discovery of daclatasvir (BMS-790052), a compound that has demonstrated clinical proof-of-concept for inhibiting the NS5A replication complex in the treatment of HCV infection...
  12. pmc Effect on hepatitis C virus replication of combinations of direct-acting antivirals, including NS5A inhibitor daclatasvir
    Lenore A Pelosi
    Department of Virology, Bristol Myers Squibb Research and Development, Wallingford, Connecticut, USA
    Antimicrob Agents Chemother 56:5230-9. 2012
    ....
  13. doi request reprint The effects of NS5A inhibitors on NS5A phosphorylation, polyprotein processing and localization
    Dike Qiu
    Department of Virology, Bristol Myers Squibb Research and Development, Wallingford, CT, USA
    J Gen Virol 92:2502-11. 2011
    ..Collectively, our results suggest that NS5A inhibitors probably impact several aspects of HCV expression and regulation. These findings may help to explain the exceptional potency of this class of HCV replication complex inhibitors...
  14. doi request reprint Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect
    Min Gao
    Department of Virology, Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, USA
    Nature 465:96-100. 2010
    ....
  15. ncbi request reprint Replication-competent chimeric hepatitis C virus subgenomic replicons
    Julie A Lemm
    Department of Virology, Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, Conn 06492, USA
    Intervirology 48:183-91. 2005
    ..To utilize chimeric hepatitis C virus (HCV) replicons to select adaptive mutation(s) that allow replication of a genotype 1a replicon...
  16. pmc Discovery of potent hepatitis C virus NS5A inhibitors with dimeric structures
    Julie A Lemm
    Department of Virology, Bristol Myers Squibb Research, 5 Research Parkway, Wallingford, Connecticut 06492, USA
    Antimicrob Agents Chemother 55:3795-802. 2011
    ..This culminated in the identification of BMS-790052, a compound that preserves the symmetry discovered with BMS-346...
  17. doi request reprint Synthesis and SAR studies of novel heteroaryl fused tetracyclic indole-diamide compounds: potent allosteric inhibitors of the hepatitis C virus NS5B polymerase
    Min Ding
    Molecular Sciences and Candidate Optimization, Bristol Myers Squibb, Research and Development, Wallingford, CT 06492, United States
    Bioorg Med Chem Lett 22:2866-71. 2012
    ....
  18. pmc Combinations of lambda interferon with direct-acting antiviral agents are highly efficient in suppressing hepatitis C virus replication
    Jacques Friborg
    Discovery Virology, Bristol Myers Squibb Research and Development, Wallingford, CT, USA
    Antimicrob Agents Chemother 57:1312-22. 2013
    ..Overall, these data support further clinical development of lambda as part of alternative combination treatments with DAAs for patients chronically infected with HCV...
  19. doi request reprint Resensitizing daclatasvir-resistant hepatitis C variants by allosteric modulation of NS5A
    Jin Hua Sun
    Department of Virology, Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, USA
    Nature 527:245-8. 2015
    ..This unprecedented synergistic anti-HCV activity also enhances the resistance barrier of DCV, providing additional options for HCV combination therapy and new insight into the role of NS5A in the HCV replication cycle. ..
  20. doi request reprint Discovery and preclinical evaluation of potent, orally bioavailable, metabolically stable cyclopropylindolobenzazepine acylsulfonamides as thumb site 1 inhibitors of the hepatitis c virus NS5B RNA-dependent, RNA polymerase
    Piyasena Hewawasam
    Department of Discovery Chemistry, Bristol Myers Squibb Pharmaceutical Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States Electronic address
    Bioorg Med Chem Lett 26:936-40. 2016
    ..Optimization of SAR, metabolic stability and PK led to the identification of compound 19 which was advanced into pre-IND enabling toxicology studies. ..
  21. pmc Specific inhibition of bovine viral diarrhea virus replicase
    Jin Hua Sun
    Department of Virology, Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492, USA
    J Virol 77:6753-60. 2003
    ..This work presents a novel inhibitor of a viral RNA-dependent RNA replicase...
  22. pmc Potency and resistance analysis of hepatitis C virus NS5B polymerase inhibitor BMS-791325 on all major genotypes
    Mengping Liu
    Department of Virology, Bristol Myers Squibb Research and Development, Wallingford, Connecticut, USA
    Antimicrob Agents Chemother 58:7416-23. 2014
    ..The results from this report suggest that BMS-791325 is a candidate for combination treatment of HCV GT3 to -6 chronic infections, and the resistance profiles identified will provide useful information for future clinical development...
  23. doi request reprint Identification of a novel series of potent HCV NS5B Site I inhibitors
    Kyle J Eastman
    Research and Development, Bristol Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA Electronic address
    Bioorg Med Chem Lett 24:1993-7. 2014
    ..Additionally, improved exposure in rats was achieved through the employment of two newly invented and now readily accessible carbon bridged propellanes as compared to their heteroatom bridged analogs...