Kyle A Emmitte

Summary

Affiliation: Vanderbilt University
Country: USA

Publications

  1. ncbi Discovery of thiophene inhibitors of polo-like kinase
    Kyle A Emmitte
    Oncology R and D, GlaxoSmithKline, Five Moore Drive, PO Box 13398, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 19:1018-21. 2009
  2. ncbi Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R)
    Kyle A Emmitte
    GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 19:1004-8. 2009
  3. ncbi Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding
    Kyle A Emmitte
    Five Moore Drive, Research Triangle Park, NC 27709, GlaxoSmithKline, USA
    Bioorg Med Chem Lett 19:1694-7. 2009
  4. ncbi In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1
    Timothy J Lansing
    GlaxoSmithKline R and D, 5 Moore Drive, Research Triangle Park, NC 27709, USA
    Mol Cancer Ther 6:450-9. 2007
  5. ncbi Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase
    Peter Sabbatini
    GlaxoSmithKline, Oncology R and D, Collegeville, PA, USA
    Clin Cancer Res 15:3058-67. 2009

Collaborators

Detail Information

Publications5

  1. ncbi Discovery of thiophene inhibitors of polo-like kinase
    Kyle A Emmitte
    Oncology R and D, GlaxoSmithKline, Five Moore Drive, PO Box 13398, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 19:1018-21. 2009
    ..The discovery and development of a series of thiophenes as potent and selective inhibitors of PLK is described. Identification and characterization of 2, a useful in vitro PLK inhibitor tool compound, is also presented...
  2. ncbi Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R)
    Kyle A Emmitte
    GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 19:1004-8. 2009
    ..Further optimization of oral exposure in mice is also discussed. Detailed selectivity, in vitro activity, and in vivo PK profiles of an optimized compound is also highlighted...
  3. ncbi Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding
    Kyle A Emmitte
    Five Moore Drive, Research Triangle Park, NC 27709, GlaxoSmithKline, USA
    Bioorg Med Chem Lett 19:1694-7. 2009
    ..Interesting selectivity between PLK1 and PLK3 was also obtained through these modifications...
  4. ncbi In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1
    Timothy J Lansing
    GlaxoSmithKline R and D, 5 Moore Drive, Research Triangle Park, NC 27709, USA
    Mol Cancer Ther 6:450-9. 2007
    ..In addition to its potential as a therapeutic agent for treating cancer, compound 1 is also a useful tool molecule for further investigation of the biological functions of PLK1 and PLK3...
  5. ncbi Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase
    Peter Sabbatini
    GlaxoSmithKline, Oncology R and D, Collegeville, PA, USA
    Clin Cancer Res 15:3058-67. 2009
    ..Agents that inhibit IGF-IR activity may be useful in treatment of patients with various cancers...