J Steven Jacobsen

Summary

Affiliation: Wyeth Research
Country: USA

Publications

  1. ncbi Acute gamma-secretase inhibition improves contextual fear conditioning in the Tg2576 mouse model of Alzheimer's disease
    Thomas A Comery
    Discovery Neuroscience, Wyeth Research, CN8000, Princeton, New Jersey 08543, USA
    J Neurosci 25:8898-902. 2005
  2. ncbi Alzheimer's disease: an overview of current and emerging therapeutic strategies
    J Steven Jacobsen
    Neuroscience Discovery Research, Wyeth Research, CN 8000, Princeton, New Jersey, 08543 8000, USA
    Curr Top Med Chem 2:343-52. 2002
  3. pmc Enhanced clearance of Abeta in brain by sustaining the plasmin proteolysis cascade
    J Steven Jacobsen
    Departments of Discovery Neuroscience and Chemical and Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
    Proc Natl Acad Sci U S A 105:8754-9. 2008
  4. pmc Early-onset behavioral and synaptic deficits in a mouse model of Alzheimer's disease
    J Steven Jacobsen
    Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
    Proc Natl Acad Sci U S A 103:5161-6. 2006
  5. doi Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease
    Robert L Martone
    Wyeth Research, Departments of Discovery Neuroscience, Princeton, New Jersey 08543, USA
    J Pharmacol Exp Ther 331:598-608. 2009
  6. doi (S)-N-(5-Chlorothiophene-2-sulfonyl)-beta,beta-diethylalaninol a Notch-1-sparing gamma-secretase inhibitor
    Derek C Cole
    Chemical and Screening Sciences, Wyeth Research, Pearl River, NY 10965, USA
    Bioorg Med Chem Lett 19:926-9. 2009
  7. doi Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease
    Scott C Mayer
    Chemical and Screening Sciences, and Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, New Jersey 08543, USA
    J Med Chem 51:7348-51. 2008
  8. ncbi Functional characterization of Narc 1, a novel proteinase related to proteinase K
    Saule Naureckiene
    Neuroscience Discovery Research, Wyeth Research, CN 8000, Princeton, NJ 08543 8000, USA
    Arch Biochem Biophys 420:55-67. 2003
  9. ncbi Expression of NALP1 in cerebellar granule neurons stimulates apoptosis
    Feng Liu
    Wyeth Neuroscience Discovery Research, CN 8000, Princeton, NJ 08543, USA
    Cell Signal 16:1013-21. 2004
  10. pmc Current concepts in therapeutic strategies targeting cognitive decline and disease modification in Alzheimer's disease
    J Steven Jacobsen
    Wyeth Research, Neuroscience Discovery, CN8000, Princeton, New Jersey 08543, USA
    NeuroRx 2:612-26. 2005

Collaborators

Detail Information

Publications12

  1. ncbi Acute gamma-secretase inhibition improves contextual fear conditioning in the Tg2576 mouse model of Alzheimer's disease
    Thomas A Comery
    Discovery Neuroscience, Wyeth Research, CN8000, Princeton, New Jersey 08543, USA
    J Neurosci 25:8898-902. 2005
    ..Furthermore, they suggest that acute treatment with GSI may provide improved cognitive functioning as well as disease-modifying effects in Alzheimer's disease...
  2. ncbi Alzheimer's disease: an overview of current and emerging therapeutic strategies
    J Steven Jacobsen
    Neuroscience Discovery Research, Wyeth Research, CN 8000, Princeton, New Jersey, 08543 8000, USA
    Curr Top Med Chem 2:343-52. 2002
    ....
  3. pmc Enhanced clearance of Abeta in brain by sustaining the plasmin proteolysis cascade
    J Steven Jacobsen
    Departments of Discovery Neuroscience and Chemical and Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
    Proc Natl Acad Sci U S A 105:8754-9. 2008
    ....
  4. pmc Early-onset behavioral and synaptic deficits in a mouse model of Alzheimer's disease
    J Steven Jacobsen
    Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
    Proc Natl Acad Sci U S A 103:5161-6. 2006
    ..Overall, these data show that the perforant path input from the entorhinal cortex to the DG is compromised both structurally and functionally, and this pathology is manifested in memory defects long before significant plaque deposition...
  5. doi Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease
    Robert L Martone
    Wyeth Research, Departments of Discovery Neuroscience, Princeton, New Jersey 08543, USA
    J Pharmacol Exp Ther 331:598-608. 2009
    ..In healthy human volunteers, oral administration of a single dose of GSI-953 produces dose-dependent changes in plasma Abeta levels, confirming pharmacodynamic activity of GSI-953 in humans...
  6. doi (S)-N-(5-Chlorothiophene-2-sulfonyl)-beta,beta-diethylalaninol a Notch-1-sparing gamma-secretase inhibitor
    Derek C Cole
    Chemical and Screening Sciences, Wyeth Research, Pearl River, NY 10965, USA
    Bioorg Med Chem Lett 19:926-9. 2009
    ..5-fold) gamma-secretase inhibitor (S)-N-(5-chlorothiophene-2-sulfonyl)-beta,beta-diethylalaninol 7.b.2 (Abeta(40/42) EC(50)=28 nM), which is efficacious in reduction of Abeta production in vivo...
  7. doi Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease
    Scott C Mayer
    Chemical and Screening Sciences, and Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, New Jersey 08543, USA
    J Med Chem 51:7348-51. 2008
    ..Further side chain modification afforded the potent Notch-1-sparing GSI begacestat (5), which was selected for development for the treatment of Alzheimer's disease...
  8. ncbi Functional characterization of Narc 1, a novel proteinase related to proteinase K
    Saule Naureckiene
    Neuroscience Discovery Research, Wyeth Research, CN 8000, Princeton, NJ 08543 8000, USA
    Arch Biochem Biophys 420:55-67. 2003
    ....
  9. ncbi Expression of NALP1 in cerebellar granule neurons stimulates apoptosis
    Feng Liu
    Wyeth Neuroscience Discovery Research, CN 8000, Princeton, NJ 08543, USA
    Cell Signal 16:1013-21. 2004
    ..Also described here are studies on the mechanism of action studies including deletion analyses and investigations of nucleotide binding, which begin to elucidate a regulatory function for NALP1 in neuronal apoptosis...
  10. pmc Current concepts in therapeutic strategies targeting cognitive decline and disease modification in Alzheimer's disease
    J Steven Jacobsen
    Wyeth Research, Neuroscience Discovery, CN8000, Princeton, New Jersey 08543, USA
    NeuroRx 2:612-26. 2005
    ....
  11. ncbi Proapoptotic effects of NARC 1 (= PCSK9), the gene encoding a novel serine proteinase
    Brendan Bingham
    Neuroscience Discovery Research, Wyeth Research, Princeton, New Jersey 08543 8000, USA
    Cytometry A 69:1123-31. 2006
    ..Coregulation of known apoptotic mediators (caspase-3 and death receptor 6) raises the possibility that NARC 1 might be involved in the propagation of apoptotic signaling in neurons...
  12. doi Antibody capture of soluble Abeta does not reduce cortical Abeta amyloidosis in the PDAPP mouse
    Peter Seubert
    Elan Pharmaceuticals, Inc, South San Francisco, Calif 94080, USA
    Neurodegener Dis 5:65-71. 2008
    ....