Mike Westby

Summary

Affiliation: Pfizer Global Research and Development
Country: USA

Publications

  1. ncbi CCR5 antagonists: host-targeted antivirals for the treatment of HIV infection
    Mike Westby
    Pfizer Global R and D, Kent, UK
    Antivir Chem Chemother 16:339-54. 2005
  2. pmc HIV-1 predisposed to acquiring resistance to maraviroc (MVC) and other CCR5 antagonists in vitro has an inherent, low-level ability to utilize MVC-bound CCR5 for entry
    Michael Roche
    Center for Virology, Burnet Institute, Melbourne, Victoria, Australia
    Retrovirology 8:89. 2011
  3. pmc Emergence of CXCR4-using human immunodeficiency virus type 1 (HIV-1) variants in a minority of HIV-1-infected patients following treatment with the CCR5 antagonist maraviroc is from a pretreatment CXCR4-using virus reservoir
    Mike Westby
    Pfizer Global Research and Development, Sandwich, United Kingdom
    J Virol 80:4909-20. 2006
  4. pmc Reduced maximal inhibition in phenotypic susceptibility assays indicates that viral strains resistant to the CCR5 antagonist maraviroc utilize inhibitor-bound receptor for entry
    Mike Westby
    Globel Research and Development, Pfizer Ltd, Sandwich Labs, Ramsgate Road, Sandwich, Kent CT13 9NJ, United Kingdom
    J Virol 81:2359-71. 2007
  5. doi CCR5 antagonists: host-targeted antiviral agents for the treatment of HIV infection, 4 years on
    Mike Westby
    Pfizer Global Research and Development, Sandwich, Kent, UK
    Antivir Chem Chemother 20:179-92. 2010
  6. doi Optimization of 5-aryloxyimidazole non-nucleoside reverse transcriptase inhibitors
    Lyn H Jones
    Discovery Chemistry, Sandwich Laboratories, Pfizer Global Research and Development, Ramsgate Road, Kent, UK
    ChemMedChem 3:1756-62. 2008
  7. pmc Characterization of resistance to the nonnucleoside NS5B inhibitor filibuvir in hepatitis C virus-infected patients
    Philip J F Troke
    Pfizer Global Research, Sandwich, Kent, United Kingdom
    Antimicrob Agents Chemother 56:1331-41. 2012
  8. pmc Small molecules targeting hepatitis C virus-encoded NS5A cause subcellular redistribution of their target: insights into compound modes of action
    Paul Targett-Adams
    Pfizer Global Research and Development, Sandwich, Kent CT13 9NJ, United Kingdom
    J Virol 85:6353-68. 2011
  9. pmc Maraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity
    Patrick Dorr
    Discovery Biology, Pfizer Global Research and Development Sandwich Laboratories, Kent CT13 9NJ, United Kingdom
    Antimicrob Agents Chemother 49:4721-32. 2005
  10. ncbi The Discovery of Potent Nonstructural Protein 5A (NS5A) Inhibitors with a Unique Resistance Profile-Part 2
    Florian Wakenhut
    Worldwide Medicinal Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ UK
    ChemMedChem 9:1387-96. 2014

Detail Information

Publications23

  1. ncbi CCR5 antagonists: host-targeted antivirals for the treatment of HIV infection
    Mike Westby
    Pfizer Global R and D, Kent, UK
    Antivir Chem Chemother 16:339-54. 2005
    ....
  2. pmc HIV-1 predisposed to acquiring resistance to maraviroc (MVC) and other CCR5 antagonists in vitro has an inherent, low-level ability to utilize MVC-bound CCR5 for entry
    Michael Roche
    Center for Virology, Burnet Institute, Melbourne, Victoria, Australia
    Retrovirology 8:89. 2011
    ..However, the CCR5-using CC1/85 strain appears to be uniquely predisposed to acquiring resistance to several CCR5 antagonists in vitro including MVC, vicriviroc and AD101...
  3. pmc Emergence of CXCR4-using human immunodeficiency virus type 1 (HIV-1) variants in a minority of HIV-1-infected patients following treatment with the CCR5 antagonist maraviroc is from a pretreatment CXCR4-using virus reservoir
    Mike Westby
    Pfizer Global Research and Development, Sandwich, United Kingdom
    J Virol 80:4909-20. 2006
    ..Importantly, in all three patients, circulating virus reverted to predominantly CCR5 tropic following cessation of maraviroc...
  4. pmc Reduced maximal inhibition in phenotypic susceptibility assays indicates that viral strains resistant to the CCR5 antagonist maraviroc utilize inhibitor-bound receptor for entry
    Mike Westby
    Globel Research and Development, Pfizer Ltd, Sandwich Labs, Ramsgate Road, Sandwich, Kent CT13 9NJ, United Kingdom
    J Virol 81:2359-71. 2007
    ..This hypothesis was further corroborated by the observation that a high concentration of maraviroc blocks the activity of aplaviroc against maraviroc-resistant virus...
  5. doi CCR5 antagonists: host-targeted antiviral agents for the treatment of HIV infection, 4 years on
    Mike Westby
    Pfizer Global Research and Development, Sandwich, Kent, UK
    Antivir Chem Chemother 20:179-92. 2010
    ..In this follow-up review, we revisit the field and assess the clinical and virological data that have emerged in the 4 years since, with particular reference to maraviroc for which the most comprehensive data currently exist...
  6. doi Optimization of 5-aryloxyimidazole non-nucleoside reverse transcriptase inhibitors
    Lyn H Jones
    Discovery Chemistry, Sandwich Laboratories, Pfizer Global Research and Development, Ramsgate Road, Kent, UK
    ChemMedChem 3:1756-62. 2008
    ..Subtle structural changes were used to probe structure-activity relationships relating to both potency and metabolic stability, which led to an imidazole derivative with an impressive overall profile...
  7. pmc Characterization of resistance to the nonnucleoside NS5B inhibitor filibuvir in hepatitis C virus-infected patients
    Philip J F Troke
    Pfizer Global Research, Sandwich, Kent, United Kingdom
    Antimicrob Agents Chemother 56:1331-41. 2012
    ..Amino acid variants at position M423 in HCV NS5B polymerase are the preferred pathway for selection of viral resistance to filibuvir in vivo...
  8. pmc Small molecules targeting hepatitis C virus-encoded NS5A cause subcellular redistribution of their target: insights into compound modes of action
    Paul Targett-Adams
    Pfizer Global Research and Development, Sandwich, Kent CT13 9NJ, United Kingdom
    J Virol 85:6353-68. 2011
    ..Taken together, our data reveal novel biological consequences of NS5A inhibition, which may help enable the development of future assay platforms for the identification of new and/or different NS5A inhibitors...
  9. pmc Maraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity
    Patrick Dorr
    Discovery Biology, Pfizer Global Research and Development Sandwich Laboratories, Kent CT13 9NJ, United Kingdom
    Antimicrob Agents Chemother 49:4721-32. 2005
    ..Clinical trials are ongoing to further investigate the potential of using maraviroc for the treatment of HIV-1 infection and AIDS...
  10. ncbi The Discovery of Potent Nonstructural Protein 5A (NS5A) Inhibitors with a Unique Resistance Profile-Part 2
    Florian Wakenhut
    Worldwide Medicinal Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ UK
    ChemMedChem 9:1387-96. 2014
    ....
  11. doi CCR5 pharmacology methodologies and associated applications
    Roy Mansfield
    Pfizer GRD Sandwich Laboratories, Sandwich, Kent, United Kingdom
    Methods Enzymol 460:17-55. 2009
    ....
  12. doi Comparison of the non-nucleoside reverse transcriptase inhibitor lersivirine with its pyrazole and imidazole isomers
    Lyn H Jones
    Sandwich Chemistry, World Wide Medicinal Chemistry, Pfizer Ltd, Ramsgate Road, Sandwich CT13 9NJ, UK Pharmacokinetic, Dynamics and Metabolism, Pfizer Ltd, Ramsgate Road, Sandwich CT13 9NJ, UK Antiviral Biology, Pfizer Ltd, Ramsgate Road, Sandwich CT13 9NJ, UK
    Chem Biol Drug Des 77:393-7. 2011
    ..This work establishes lersivirine as the outstanding molecule in this set...
  13. ncbi The Discovery of Potent Nonstructural Protein 5A (NS5A) Inhibitors with a Unique Resistance Profile-Part 1
    Thien Duc Tran
    Worldwide Medicinal Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ UK
    ChemMedChem 9:1378-86. 2014
    ..This compound represents a promising lead that warrants further evaluation. ..
  14. doi Therapy with TLR7 agonists induces lymphopenia: correlating pharmacology to mechanism in a mouse model
    Hannah Perkins
    Pfizer Ltd, Ramsgate Road, Sandwich, Kent, UK
    J Clin Immunol 32:1082-92. 2012
    ..We wished to understand and characterise the relationship between TLR7 agonism and adverse effects...
  15. doi Colony-forming assays reveal enhanced suppression of hepatitis C virus replication using combinations of direct-acting antivirals
    Emily J S Graham
    Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, Kent CT13 9NJ, UK
    J Virol Methods 174:153-7. 2011
    ..Collectively, these data underscore the increased inhibitory capacity of direct-acting antivirals to suppress HCV RNA replication when present in combination...
  16. doi An imidazopiperidine series of CCR5 antagonists for the treatment of HIV: the discovery of N-{(1S)-1-(3-fluorophenyl)-3-[(3-endo)-3-(5-isobutyryl-2-methyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]oct-8-yl]propyl}acetamide (PF-2
    Paul A Stupple
    Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, Kent, United Kingdom
    J Med Chem 54:67-77. 2011
    ..Compound 41f (PF-232798) was selected as a clinical candidate from the imidazopiperidine series and is currently in phase II clinical trials...
  17. ncbi A pharmacokinetic-pharmacodynamic model to optimize the phase IIa development program of maraviroc
    Maria C Rosario
    Department of Clinical Pharmacology, Pfizer Clinical R and D, Groton, CT 06340, USA
    J Acquir Immune Defic Syndr 42:183-91. 2006
    ....
  18. pmc Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1
    Romuald Corbau
    Department of Discovery Biology, Pfizer Global Research and Development, Sandwich, Kent CT13 9NJ, United Kingdom
    Antimicrob Agents Chemother 54:4451-63. 2010
    ..Altogether lersivirine is a highly potent and selective NNRTI, with excellent efficacy against NNRTI-resistant viruses...
  19. pmc Knockdown of USP18 increases α 2a interferon signaling and induction of interferon-stimulating genes but does not increase antiviral activity in Huh7 cells
    E J Murray
    Internal Medicine, IPC 424, Pfizer PGRD, Discovery Biology, Sandwich Laboratories, Sandwich, Kent CT13 9NJ, United Kingdom
    Antimicrob Agents Chemother 55:4311-9. 2011
    ..5 cells. These data suggest that the IFN-mediated AV response in Huh7.5 cells has only a limited dependence on USP18 activity...
  20. pmc Use of a highly sensitive strand-specific quantitative PCR to identify abortive replication in the mouse model of respiratory syncytial virus disease
    Richard Bannister
    Infectious Diseases Group, Pfizer Global Research and Development, Sandwich, Kent CT13 9NJ, UK
    Virol J 7:250. 2010
    ....
  21. doi Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays
    Lyn H Jones
    Discovery Chemistry, Sandwich Laboratories, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, United Kingdom
    J Med Chem 52:1219-23. 2009
    ....
  22. ncbi Cell-based and biochemical screening approaches for the discovery of novel HIV-1 inhibitors
    Mike Westby
    Antiinfectives Biology, Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road Sandwich, Kent CT13 9NJ, UK
    Antiviral Res 67:121-40. 2005
    ..As drug discovery efforts in the pharmaceutical industry shift away from traditional strategies, new approaches such as those presented here are likely to play a significant role in the identification of next generation HIV-1 inhibitors...
  23. doi Subgroup analyses of maraviroc in previously treated R5 HIV-1 infection
    Gerd Fatkenheuer
    Universitätsklinik Köln, Cologne, Germany
    N Engl J Med 359:1442-55. 2008
    ....