Guriqbal S Basi

Summary

Affiliation: Elan Pharmaceuticals
Country: USA

Publications

  1. ncbi request reprint Amyloid beta-protein precursor juxtamembrane domain regulates specificity of gamma-secretase-dependent cleavages
    Zhao Ren
    Elan Pharmaceuticals, Inc, South San Francisco, California 94080, USA
    J Biol Chem 282:35350-60. 2007
  2. doi request reprint Discovery of sulfonamide-pyrazole gamma-secretase inhibitors
    Matthew N Mattson
    Elan Pharmaceuticals, 800 Gateway Blvd, South San Francisco, CA 94080, United States
    Bioorg Med Chem Lett 20:2148-50. 2010
  3. pmc Evidence that enzyme processivity mediates differential Aβ production by PS1 and PS2
    Sean A Pintchovski
    Elan Pharmaceuticals, Inc, 180 Oyster Pt Blvd, South San Francisco, CA 94080, USA
    Curr Alzheimer Res 10:4-10. 2013
  4. pmc Structural correlates of antibodies associated with acute reversal of amyloid beta-related behavioral deficits in a mouse model of Alzheimer disease
    Guriqbal S Basi
    Elan Pharmaceuticals, Incorporated, South San Francisco, California 94080, USA
    J Biol Chem 285:3417-27. 2010
  5. doi request reprint Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007
    Gary Probst
    Department of Medicinal Chemistry, Elan Pharmaceuticals, 180 Oyster Point Boulevard, South San Francisco, California 94080, United States
    J Med Chem 56:5261-74. 2013
  6. doi request reprint Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors
    Xiaocong M Ye
    Department of Medicinal Chemistry, Elan Pharmaceuticals, 180 Oyster Point Blvd, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 23:996-1000. 2013
  7. doi request reprint Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors (Part II)
    Xiaocong M Ye
    Department of Medicinal Chemistry, Elan Pharmaceuticals, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 20:3502-6. 2010
  8. doi request reprint Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors
    Xiaocong M Ye
    Department of Medicinal Chemistry, Elan Pharmaceuticals, 800 Gateway Boulevard, South San Francisco, CA 94080, United States
    Bioorg Med Chem Lett 20:2195-9. 2010
  9. pmc Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease
    Guriqbal S Basi
    Elan Pharmaceuticals, Inc, 180 Oyster Point Blvd, S, San Francisco, CA 94080, USA
    Alzheimers Res Ther 2:36. 2010
  10. doi request reprint N-Bridged bicyclic sulfonamides as inhibitors of gamma-secretase
    Simeon Bowers
    Department of Medicinal Chemistry, Elan Pharmaceuticals, 800 Gateway Boulevard, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 19:6952-6. 2009

Collaborators

Detail Information

Publications11

  1. ncbi request reprint Amyloid beta-protein precursor juxtamembrane domain regulates specificity of gamma-secretase-dependent cleavages
    Zhao Ren
    Elan Pharmaceuticals, Inc, South San Francisco, California 94080, USA
    J Biol Chem 282:35350-60. 2007
    ..These results indicate that the luminal juxtamembrane region of APP is an important regulatory domain that modulates gamma-secretase-dependent intramembrane proteolysis, particularly in differentiating gamma- and epsilon-cleavages...
  2. doi request reprint Discovery of sulfonamide-pyrazole gamma-secretase inhibitors
    Matthew N Mattson
    Elan Pharmaceuticals, 800 Gateway Blvd, South San Francisco, CA 94080, United States
    Bioorg Med Chem Lett 20:2148-50. 2010
    ....
  3. pmc Evidence that enzyme processivity mediates differential Aβ production by PS1 and PS2
    Sean A Pintchovski
    Elan Pharmaceuticals, Inc, 180 Oyster Pt Blvd, South San Francisco, CA 94080, USA
    Curr Alzheimer Res 10:4-10. 2013
    ..Taken together these findings offer novel insights into γ- secretase biology and have important implications for therapeutically targeting γ-secretase...
  4. pmc Structural correlates of antibodies associated with acute reversal of amyloid beta-related behavioral deficits in a mouse model of Alzheimer disease
    Guriqbal S Basi
    Elan Pharmaceuticals, Incorporated, South San Francisco, California 94080, USA
    J Biol Chem 285:3417-27. 2010
    ..These findings provide a structural basis for immunotherapeutic strategies targeting Abeta species postulated to underlie cognitive deficits in AD...
  5. doi request reprint Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007
    Gary Probst
    Department of Medicinal Chemistry, Elan Pharmaceuticals, 180 Oyster Point Boulevard, South San Francisco, California 94080, United States
    J Med Chem 56:5261-74. 2013
    ..A comparison of inhibition of Aβ generation in vivo between 30, 34, Semagacestat 41, Begacestat 42, and Avagacestat 43 in mice is made. 30 lowered Aβ in the CSF of healthy human volunteers...
  6. doi request reprint Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors
    Xiaocong M Ye
    Department of Medicinal Chemistry, Elan Pharmaceuticals, 180 Oyster Point Blvd, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 23:996-1000. 2013
    ..Compounds that are efficacious in reducing the cortical Aβx-40 levels in FVB mice via oral dose, as well as those with high selectivity over Notch, are highlighted...
  7. doi request reprint Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors (Part II)
    Xiaocong M Ye
    Department of Medicinal Chemistry, Elan Pharmaceuticals, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 20:3502-6. 2010
    ..Significant improvement in metabolic stability on the pyrazolopiperidine scaffold over the original series were achieved and this stability improvement translated in an improved in vivo efficacy...
  8. doi request reprint Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors
    Xiaocong M Ye
    Department of Medicinal Chemistry, Elan Pharmaceuticals, 800 Gateway Boulevard, South San Francisco, CA 94080, United States
    Bioorg Med Chem Lett 20:2195-9. 2010
    ..Significant increases in APP potency on the pyrazolopiperidine scaffold over the original N-bicyclic sulfonamide scaffold were achieved and this potency increase translated in an improved in vivo efficacy...
  9. pmc Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease
    Guriqbal S Basi
    Elan Pharmaceuticals, Inc, 180 Oyster Point Blvd, S, San Francisco, CA 94080, USA
    Alzheimers Res Ther 2:36. 2010
    ..It has been postulated that APP substrate selective inhibitors of gamma-secretase would be preferable to non-selective inhibitors from a safety perspective for AD therapy...
  10. doi request reprint N-Bridged bicyclic sulfonamides as inhibitors of gamma-secretase
    Simeon Bowers
    Department of Medicinal Chemistry, Elan Pharmaceuticals, 800 Gateway Boulevard, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 19:6952-6. 2009
    ..Appropriate substitution on the bicyclic scaffold provides a significant increase in the metabolic stability of the compounds resulting in an improved in vivo metabolic profile...
  11. pmc Treatment strategies targeting amyloid β-protein
    Dale Schenk
    Netotope Biosciences Inc, San Francisco, CA 94080, USA
    Cold Spring Harb Perspect Med 2:a006387. 2012
    ..Here we review the progress in this field toward the goal of targeting Aβ for treatment and prevention of AD and identify some of the major challenges for the future of this area of medicine...