Norman C Waters

Summary

Affiliation: Walter Reed Army Medical Center
Country: USA

Publications

  1. ncbi request reprint Targeting protein kinases in the malaria parasite: update of an antimalarial drug target
    Veronica M Zhang
    Australian Army Malaria Institute, Gallipoli Barracks, Enoggera, QLD
    Curr Top Med Chem 12:456-72. 2012
  2. pmc Increased prevalence of the pfdhfr/phdhps quintuple mutant and rapid emergence of pfdhps resistance mutations at codons 581 and 613 in Kisumu, Kenya
    Maroya D Spalding
    Department of Epidemiology, Johns Hopkins Bloomberg School of Public Health, Baltimore, Maryland, USA
    Malar J 9:338. 2010
  3. ncbi request reprint Exploring novel targets for antimalarial drug discovery: plasmodial protein kinases
    Dayadevi Jirage
    Department of Parasitology, Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, USA
    Infect Disord Drug Targets 10:134-46. 2010
  4. doi request reprint Selective inhibition of Pfmrk, a Plasmodium falciparum CDK, by antimalarial 1,3-diaryl-2-propenones
    Jeanne A Geyer
    Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, MD 20910, United States
    Bioorg Med Chem Lett 19:1982-5. 2009
  5. ncbi request reprint A three-dimensional in silico pharmacophore model for inhibition of Plasmodium falciparum cyclin-dependent kinases and discovery of different classes of novel Pfmrk specific inhibitors
    Apurba K Bhattacharjee
    Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910 7500, USA
    J Med Chem 47:5418-26. 2004
  6. pmc Assessment of malaria in vitro drug combination screening and mixed-strain infections using the malaria Sybr green I-based fluorescence assay
    Edgie Mark A Co
    Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, MD 20910, USA
    Antimicrob Agents Chemother 53:2557-63. 2009
  7. ncbi request reprint Evaluation of broad spectrum protein kinase inhibitors to probe the architecture of the malarial cyclin dependent protein kinase Pfmrk
    Cassandra L Woodard
    Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, MD 20910, USA
    Bioorg Med Chem Lett 17:4961-6. 2007
  8. ncbi request reprint Identification of an effector protein and gain-of-function mutants that activate Pfmrk, a malarial cyclin-dependent protein kinase
    Yueqin Chen
    Department of Parasitology, Division of Experimental Therapeutics, Walter Reed Army Institute of Research, 503 Robert Grant Avenue, Silver Spring, MD 20910, USA
    Mol Biochem Parasitol 149:48-57. 2006
  9. doi request reprint The malarial CDK Pfmrk and its effector PfMAT1 phosphorylate DNA replication proteins and co-localize in the nucleus
    Dayadevi Jirage
    Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, MD 20910, USA
    Mol Biochem Parasitol 172:9-18. 2010
  10. doi request reprint Activity of substituted thiophene sulfonamides against malarial and mammalian cyclin dependent protein kinases
    Diana Caridha
    Walter Reed Army Institute of Research, Silver Spring, MD 20910, USA
    Bioorg Med Chem Lett 20:3863-7. 2010

Collaborators

Detail Information

Publications15

  1. ncbi request reprint Targeting protein kinases in the malaria parasite: update of an antimalarial drug target
    Veronica M Zhang
    Australian Army Malaria Institute, Gallipoli Barracks, Enoggera, QLD
    Curr Top Med Chem 12:456-72. 2012
    ..As the search for novel antimalarials continues, an understanding of the phosphor-regulatory pathways will not only validate protein kinase targets, but also will identify novel chemotypes to thwart malaria drug resistance...
  2. pmc Increased prevalence of the pfdhfr/phdhps quintuple mutant and rapid emergence of pfdhps resistance mutations at codons 581 and 613 in Kisumu, Kenya
    Maroya D Spalding
    Department of Epidemiology, Johns Hopkins Bloomberg School of Public Health, Baltimore, Maryland, USA
    Malar J 9:338. 2010
    ..The baseline study was carried out from 1999-2000, shortly after implementation of SP, and the follow-up study occurred from 2003-2005, during the transition to AL...
  3. ncbi request reprint Exploring novel targets for antimalarial drug discovery: plasmodial protein kinases
    Dayadevi Jirage
    Department of Parasitology, Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, USA
    Infect Disord Drug Targets 10:134-46. 2010
    ..With wide spread malaria drug resistance, coupled by a parasite that can develop resistance quickly to new drugs, the development of multi-kinase inhibitors may be extremely efficacious and reduce the likelihood for resistance...
  4. doi request reprint Selective inhibition of Pfmrk, a Plasmodium falciparum CDK, by antimalarial 1,3-diaryl-2-propenones
    Jeanne A Geyer
    Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, MD 20910, United States
    Bioorg Med Chem Lett 19:1982-5. 2009
    ..Several mechanisms of action have been suggested for chalcone derivatives and our study suggests that kinase inhibition may be an additional mechanism of antimalarial activity for this class of compounds...
  5. ncbi request reprint A three-dimensional in silico pharmacophore model for inhibition of Plasmodium falciparum cyclin-dependent kinases and discovery of different classes of novel Pfmrk specific inhibitors
    Apurba K Bhattacharjee
    Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910 7500, USA
    J Med Chem 47:5418-26. 2004
    ..The predicted inhibitory activities of some of these Pfmrk inhibitors from the molecular model agree exceptionally well with the experimental inhibitory values from the in vitro CDK assay...
  6. pmc Assessment of malaria in vitro drug combination screening and mixed-strain infections using the malaria Sybr green I-based fluorescence assay
    Edgie Mark A Co
    Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, MD 20910, USA
    Antimicrob Agents Chemother 53:2557-63. 2009
    ..In conclusion, the MSF assay allows for reliable antimalarial drug combination screening and provides an important method to discern between homogenous and heterogeneous parasite populations...
  7. ncbi request reprint Evaluation of broad spectrum protein kinase inhibitors to probe the architecture of the malarial cyclin dependent protein kinase Pfmrk
    Cassandra L Woodard
    Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, MD 20910, USA
    Bioorg Med Chem Lett 17:4961-6. 2007
    ..Structural analysis suggests that even subtle differences in amino acid composition within the active sites are responsible for conferring specificity of these inhibitors for Pfmrk over PKA...
  8. ncbi request reprint Identification of an effector protein and gain-of-function mutants that activate Pfmrk, a malarial cyclin-dependent protein kinase
    Yueqin Chen
    Department of Parasitology, Division of Experimental Therapeutics, Walter Reed Army Institute of Research, 503 Robert Grant Avenue, Silver Spring, MD 20910, USA
    Mol Biochem Parasitol 149:48-57. 2006
    ..Significant kinase activity of these mutants was observed in the absence of either cyclin or PfMAT1. Finally, we observed autophosphorylation of Pfmrk that is unaffected by the addition of either cyclin or PfMAT1...
  9. doi request reprint The malarial CDK Pfmrk and its effector PfMAT1 phosphorylate DNA replication proteins and co-localize in the nucleus
    Dayadevi Jirage
    Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, MD 20910, USA
    Mol Biochem Parasitol 172:9-18. 2010
    ..Collectively, these data suggest a role for Pfmrk in the nucleus of the parasite presumably in regulation of the DNA replication machinery...
  10. doi request reprint Activity of substituted thiophene sulfonamides against malarial and mammalian cyclin dependent protein kinases
    Diana Caridha
    Walter Reed Army Institute of Research, Silver Spring, MD 20910, USA
    Bioorg Med Chem Lett 20:3863-7. 2010
    ..These compounds represent the most potent Pfmrk inhibitors reported and provide support for further characterization and derivation as potential antimalarial agents...
  11. ncbi request reprint Recent advances in malaria drug discovery
    Charlotte A Lanteri
    Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, USA
    Recent Pat Antiinfect Drug Discov 2:95-114. 2007
    ..New approaches to drug discovery should identify novel chemotypes which circumvent the parasite's disposition to drug resistance. This review summarizes current efforts in malaria drug discovery as uncovered in recent patent literature...
  12. pmc Targeting the fatty acid biosynthesis enzyme, beta-ketoacyl-acyl carrier protein synthase III (PfKASIII), in the identification of novel antimalarial agents
    Patricia J Lee
    Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, USA
    J Med Chem 52:952-63. 2009
    ..Docking studies into the active site of PfKASIII suggest a potential binding mode that exploits amino acid residues at the mouth of the substrate tunnel...
  13. pmc Assessment and continued validation of the malaria SYBR green I-based fluorescence assay for use in malaria drug screening
    Jacob D Johnson
    Principal Investigator, Department of Parasitology, Division of Experimental Therapeutics, Walter Reed Army Institute of Research, 503 Robert Grant Ave, Silver Spring, MD 20910, USA
    Antimicrob Agents Chemother 51:1926-33. 2007
    ..In conclusion, the MSF assay allows for reliable one-plate high-throughput, automated malaria in vitro susceptibility testing without the expense, time consumption, and hazard of other screening assays...
  14. ncbi request reprint Fatty Acid synthesis as a target for antimalarial drug discovery
    Jeff Zhiqiang Lu
    Johns Hopkins University, Bloomberg School of Public Health, Department of Molecular Microbiology and Immunology, Baltimore, MD 21205, USA
    Comb Chem High Throughput Screen 8:15-26. 2005
    ..Ongoing antimalarial drug discovery projects will be described in this review as well as background information about the well-studied bacterial type II FAS enzymes...
  15. ncbi request reprint Oxindole-based compounds are selective inhibitors of Plasmodium falciparum cyclin dependent protein kinases
    Cassandra L Woodard
    Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, USA
    J Med Chem 46:3877-82. 2003
    ..Amino acid comparison of the active sites of Pfmrk and PfPK5 identified unique amino acid differences that may explain this selectivity and be exploited for further drug development efforts...