Paul M McNicholas

Summary

Affiliation: Merck Research Laboratories
Country: USA

Publications

  1. doi Mapping and characterization of vicriviroc resistance mutations from HIV-1 isolated from treatment-experienced subjects enrolled in a phase II study (VICTOR-E1)
    Paul M McNicholas
    Department of Infectious Diseases, Merck Research Labs, Kenilworth, NJ 07033, USA
    J Acquir Immune Defic Syndr 56:222-9. 2011
  2. pmc Posaconazole is a potent inhibitor of sterol 14alpha-demethylation in yeasts and molds
    Hanan K Munayyer
    Mailing address Schering Plough Research Institute, 2015 Galloping Hill Rd, K15 4 4700, Kenilworth, NJ 07033
    Antimicrob Agents Chemother 48:3690-6. 2004
  3. pmc Application of real-time quantitative PCR to molecular analysis of Candida albicans strains exhibiting reduced susceptibility to azoles
    Andrew S Chau
    Schering Plough Research Institute, 2015 Galloping Hill Rd, K15 4 4700, Kenilworth, NJ 07033, USA
    Antimicrob Agents Chemother 48:2124-31. 2004
  4. pmc Discovery of a novel class of orally active antifungal beta-1,3-D-glucan synthase inhibitors
    Scott S Walker
    Department of Infectious Diseases, Merck Research Laboratories, Kenilworth, New Jersey 07033, USA
    Antimicrob Agents Chemother 55:5099-106. 2011
  5. pmc Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species
    Paul A Mann
    Schering Plough Research Institute, Kenilworth, NJ 07033, USA
    Antimicrob Agents Chemother 53:5026-34. 2009
  6. pmc Inactivation of sterol Delta5,6-desaturase attenuates virulence in Candida albicans
    Andrew S Chau
    Schering Plough Research Institute, K15 4 4700, 2015 Galloping Hill Road, Kenilworth, NJ 07033
    Antimicrob Agents Chemother 49:3646-51. 2005
  7. ncbi Changes in susceptibility to posaconazole in clinical isolates of Candida albicans
    Xin Li
    Schering Plough Research Institute, 2015 Galloping Hill Road, 4700 Kenilworth, NJ 07033, USA
    J Antimicrob Chemother 53:74-80. 2004
  8. pmc Three-dimensional models of wild-type and mutated forms of cytochrome P450 14alpha-sterol demethylases from Aspergillus fumigatus and Candida albicans provide insights into posaconazole binding
    Li Xiao
    Department of Structural Chemistry, Schering Plough Research Institute, Kenilworth, New Jersey 07033, USA
    Antimicrob Agents Chemother 48:568-74. 2004
  9. pmc Molecular basis for enhanced activity of posaconazole against Absidia corymbifera and Rhizopus oryzae
    Andrew S Chau
    Schering Plough Research Institute, 2015 Galloping Hill Road, 4700, Kenilworth, NJ 07033, USA
    Antimicrob Agents Chemother 50:3917-9. 2006
  10. doi The synthesis and structure-activity relationship of pyridazinones as glucan synthase inhibitors
    Pauline C Ting
    Department of Chemical Research, Merck Research Laboratories, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 21:1819-22. 2011

Collaborators

Detail Information

Publications13

  1. doi Mapping and characterization of vicriviroc resistance mutations from HIV-1 isolated from treatment-experienced subjects enrolled in a phase II study (VICTOR-E1)
    Paul M McNicholas
    Department of Infectious Diseases, Merck Research Labs, Kenilworth, NJ 07033, USA
    J Acquir Immune Defic Syndr 56:222-9. 2011
    ..Among the 79 VCV-treated subjects, 15 experienced virologic failure, and of these 5 had VCV-resistant virus. This study investigated the molecular basis for the changes in susceptibility to VCV in these subjects...
  2. pmc Posaconazole is a potent inhibitor of sterol 14alpha-demethylation in yeasts and molds
    Hanan K Munayyer
    Mailing address Schering Plough Research Institute, 2015 Galloping Hill Rd, K15 4 4700, Kenilworth, NJ 07033
    Antimicrob Agents Chemother 48:3690-6. 2004
    ..In addition, POS was a more potent inhibitor of sterol synthesis in A. fumigatus and A. flavus than either ITZ or VOR...
  3. pmc Application of real-time quantitative PCR to molecular analysis of Candida albicans strains exhibiting reduced susceptibility to azoles
    Andrew S Chau
    Schering Plough Research Institute, 2015 Galloping Hill Rd, K15 4 4700, Kenilworth, NJ 07033, USA
    Antimicrob Agents Chemother 48:2124-31. 2004
    ..Despite both the increases in pump expression and the ERG11 mutations, only one of the patient isolates exhibited a large decrease in posaconazole susceptibility...
  4. pmc Discovery of a novel class of orally active antifungal beta-1,3-D-glucan synthase inhibitors
    Scott S Walker
    Department of Infectious Diseases, Merck Research Laboratories, Kenilworth, New Jersey 07033, USA
    Antimicrob Agents Chemother 55:5099-106. 2011
    ..Finally, we present efficacy and pharmacokinetic data on an example of the piperazinyl-pyridazinone compounds that demonstrated efficacy in a murine model of Candida glabrata infection...
  5. pmc Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species
    Paul A Mann
    Schering Plough Research Institute, Kenilworth, NJ 07033, USA
    Antimicrob Agents Chemother 53:5026-34. 2009
    ..Overall breakthrough infections by Candida species were very rare (approximately 1%), and C. glabrata was the colonizing species that was the most frequently associated with breakthrough infections...
  6. pmc Inactivation of sterol Delta5,6-desaturase attenuates virulence in Candida albicans
    Andrew S Chau
    Schering Plough Research Institute, K15 4 4700, 2015 Galloping Hill Road, Kenilworth, NJ 07033
    Antimicrob Agents Chemother 49:3646-51. 2005
    ..Reintroduction of a wild-type ERG3 allele into the homozygous deletion mutant restored virulence, ergosterol synthesis, and susceptibility to azoles, confirming that these phenotypic changes were solely due to the inactivation of Erg3p...
  7. ncbi Changes in susceptibility to posaconazole in clinical isolates of Candida albicans
    Xin Li
    Schering Plough Research Institute, 2015 Galloping Hill Road, 4700 Kenilworth, NJ 07033, USA
    J Antimicrob Chemother 53:74-80. 2004
    ..To characterize the molecular mechanisms responsible for reduced susceptibility to azoles in Candida albicans clinical isolates...
  8. pmc Three-dimensional models of wild-type and mutated forms of cytochrome P450 14alpha-sterol demethylases from Aspergillus fumigatus and Candida albicans provide insights into posaconazole binding
    Li Xiao
    Department of Structural Chemistry, Schering Plough Research Institute, Kenilworth, New Jersey 07033, USA
    Antimicrob Agents Chemother 48:568-74. 2004
    ..The model also predicts that mutations that were previously shown to specifically impact POS susceptibility in A. fumigatus and C. albicans act by interfering with the binding of the long side chain...
  9. pmc Molecular basis for enhanced activity of posaconazole against Absidia corymbifera and Rhizopus oryzae
    Andrew S Chau
    Schering Plough Research Institute, 2015 Galloping Hill Road, 4700, Kenilworth, NJ 07033, USA
    Antimicrob Agents Chemother 50:3917-9. 2006
    ..Similarly, expression of CYP51 from R. oryzae in Saccharomyces cerevisiae significantly increased resistance to fluconazole and voriconazole but not to posaconazole and itraconazole...
  10. doi The synthesis and structure-activity relationship of pyridazinones as glucan synthase inhibitors
    Pauline C Ting
    Department of Chemical Research, Merck Research Laboratories, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 21:1819-22. 2011
    ..Compound 11c exhibited significant efficacy in an in vivo mouse model of Candida glabrata infection...
  11. pmc Clinical evaluation of the Sensititre YeastOne plate for testing susceptibility of filamentous fungi to posaconazole
    Reena Patel
    Schering Plough Research Institute, Kenilworth, NJ 07033, USA
    J Clin Microbiol 45:2000-1. 2007
    ..These data confirm the utility of YeastOne panels for measuring the susceptibility of filamentous fungi to posaconazole...
  12. doi SAR studies of pyridazinone derivatives as novel glucan synthase inhibitors
    Gang Zhou
    Department of Chemical Research, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 21:2890-3. 2011
    ..Optimization of the sulfonamide moiety led to the identification of important compounds with much improved systematic exposure while retaining good antifungal activity against the fungal strains Candida glabrata and Candida albicans...
  13. pmc Mutations in Aspergillus fumigatus resulting in reduced susceptibility to posaconazole appear to be restricted to a single amino acid in the cytochrome P450 14alpha-demethylase
    Paul A Mann
    Schering Plough Research Institute, Kenilworth, New Jersey 07033, USA
    Antimicrob Agents Chemother 47:577-81. 2003
    ..The transformants exhibited reductions in susceptibility to POS comparable to those exhibited by the original mutants, confirming that point mutations in the cyp51A gene in A. fumigatus can confer reduced susceptibility to POS...