Stephen J Gardell

Summary

Affiliation: Wyeth Research
Country: USA

Publications

  1. ncbi request reprint Neutralization of plasminogen activator inhibitor I (PAI-1) by the synthetic antagonist PAI-749 via a dual mechanism of action
    Stephen J Gardell
    Wyeth Research, N2274, 500 Arcola Road, Collegeville, PA 19426, USA
    Mol Pharmacol 72:897-906. 2007
  2. doi request reprint A synthetic farnesoid X receptor (FXR) agonist promotes cholesterol lowering in models of dyslipidemia
    Mark J Evans
    Department of Cardiovascular and Metabolic Diseases, Wyeth Research, 500 Arcola Rd, Collegeville, PA 19426, USA
    Am J Physiol Gastrointest Liver Physiol 296:G543-52. 2009
  3. doi request reprint Selective Kv1.5 blockers: development of (R)-1-(methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a potential treatment for atrial arrhythmia
    Benjamin E Blass
    Chemical Sciences, Wyeth Research, Collegeville, Pennsylvania 19426, USA
    J Med Chem 52:6531-4. 2009
  4. doi request reprint Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis
    Jay Wrobel
    Chemical and Screening Sciences, Wyeth Pharmaceuticals, 500 Arcola Road, Collegeville, Pennsylvania 19426, USA
    J Med Chem 51:7161-8. 2008
  5. pmc LXR ligand lowers LDL cholesterol in primates, is lipid neutral in hamster, and reduces atherosclerosis in mouse
    Elaine M Quinet
    Department of Cardiovascular Metabolic Diseases and Nuclear Receptor Biology, Wyeth Research, Collegeville, PA, USA
    J Lipid Res 50:2358-70. 2009
  6. doi request reprint GAP-134 ([2S,4R]-1-[2-aminoacetyl]4-benzamidopyrrolidine-2-carboxylic acid) prevents spontaneous ventricular arrhythmias and reduces infarct size during myocardial ischemia/reperfusion injury in open-chest dogs
    James K Hennan
    Cardiovascular and Metabolic Disease Research, Collegeville, Pennsylvania, USA
    J Cardiovasc Pharmacol Ther 14:207-14. 2009
  7. doi request reprint The gap junction modifier, GAP-134 [(2S,4R)-1-(2-aminoacetyl)-4-benzamido-pyrrolidine-2-carboxylic acid], improves conduction and reduces atrial fibrillation/flutter in the canine sterile pericarditis model
    Eric I Rossman
    Cardiovascular and Metabolic Disease, Wyeth Research, Collegeville, PA 19426, USA
    J Pharmacol Exp Ther 329:1127-33. 2009
  8. pmc Activation of farnesoid X receptor prevents atherosclerotic lesion formation in LDLR-/- and apoE-/- mice
    Helen B Hartman
    Cardiovascular and Metabolic Disease Research, Wyeth Research, Collegeville, PA 19426, USA
    J Lipid Res 50:1090-100. 2009
  9. 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
  10. ncbi request reprint A presenilin-independent aspartyl protease prefers the gamma-42 site cleavage
    Ming Tain Lai
    Department of Biological Chemistry, Merck Research Laboratories, West Point, Pennsylvania, USA
    J Neurochem 96:118-25. 2006

Collaborators

Detail Information

Publications10

  1. ncbi request reprint Neutralization of plasminogen activator inhibitor I (PAI-1) by the synthetic antagonist PAI-749 via a dual mechanism of action
    Stephen J Gardell
    Wyeth Research, N2274, 500 Arcola Road, Collegeville, PA 19426, USA
    Mol Pharmacol 72:897-906. 2007
    ..Second, binding of PAI-749 to PAI-1 renders PAI-1 vulnerable to plasmin-mediated proteolytic degradation...
  2. doi request reprint A synthetic farnesoid X receptor (FXR) agonist promotes cholesterol lowering in models of dyslipidemia
    Mark J Evans
    Department of Cardiovascular and Metabolic Diseases, Wyeth Research, 500 Arcola Rd, Collegeville, PA 19426, USA
    Am J Physiol Gastrointest Liver Physiol 296:G543-52. 2009
    ..These studies demonstrate a consistent ability of WAY-362450 to lower both serum TG and cholesterol levels and suggest that synthetic FXR agonists may have clinical utility in the treatment of mixed dyslipidemia...
  3. doi request reprint Selective Kv1.5 blockers: development of (R)-1-(methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a potential treatment for atrial arrhythmia
    Benjamin E Blass
    Chemical Sciences, Wyeth Research, Collegeville, Pennsylvania 19426, USA
    J Med Chem 52:6531-4. 2009
    ..KVI-020 (4g) successfully demonstrated antiarrhythmic efficacy in a canine arrhythmia model, and these findings support its utility as an antiarrhythmic agent...
  4. doi request reprint Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis
    Jay Wrobel
    Chemical and Screening Sciences, Wyeth Pharmaceuticals, 500 Arcola Road, Collegeville, Pennsylvania 19426, USA
    J Med Chem 51:7161-8. 2008
    ..These results suggest indazoles such as 13 may have an improved profile for potential use as a therapeutic agent...
  5. pmc LXR ligand lowers LDL cholesterol in primates, is lipid neutral in hamster, and reduces atherosclerosis in mouse
    Elaine M Quinet
    Department of Cardiovascular Metabolic Diseases and Nuclear Receptor Biology, Wyeth Research, Collegeville, PA, USA
    J Lipid Res 50:2358-70. 2009
    ..WAY-252623 displays a unique and favorable pharmacological profile suggesting synthetic LXR ligands with these characteristics may be suitable for evaluation in patients with atherosclerotic dyslipidemia...
  6. doi request reprint GAP-134 ([2S,4R]-1-[2-aminoacetyl]4-benzamidopyrrolidine-2-carboxylic acid) prevents spontaneous ventricular arrhythmias and reduces infarct size during myocardial ischemia/reperfusion injury in open-chest dogs
    James K Hennan
    Cardiovascular and Metabolic Disease Research, Collegeville, Pennsylvania, USA
    J Cardiovasc Pharmacol Ther 14:207-14. 2009
    ..0% + 3.5% in controls to 7.9% + 1.5% and 7.1% + 0.8% (P < .05) at the 2 highest doses of GAP-134. GAP-134 is an effective antiarrhythmic agent with potential to reduce ischemia/reperfusion injury...
  7. doi request reprint The gap junction modifier, GAP-134 [(2S,4R)-1-(2-aminoacetyl)-4-benzamido-pyrrolidine-2-carboxylic acid], improves conduction and reduces atrial fibrillation/flutter in the canine sterile pericarditis model
    Eric I Rossman
    Cardiovascular and Metabolic Disease, Wyeth Research, Collegeville, PA 19426, USA
    J Pharmacol Exp Ther 329:1127-33. 2009
    ..These findings, along with its oral bioavailability, underscore its potential antiarrhythmic efficacy...
  8. pmc Activation of farnesoid X receptor prevents atherosclerotic lesion formation in LDLR-/- and apoE-/- mice
    Helen B Hartman
    Cardiovascular and Metabolic Disease Research, Wyeth Research, Collegeville, PA 19426, USA
    J Lipid Res 50:1090-100. 2009
    ..These results suggest that activation of FXR protects against atherosclerosis in the mouse, and this protective effect correlates with repression of bile acid synthetic genes, with mechanistic differences between male and female mice...
  9. 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
    ....
  10. ncbi request reprint A presenilin-independent aspartyl protease prefers the gamma-42 site cleavage
    Ming Tain Lai
    Department of Biological Chemistry, Merck Research Laboratories, West Point, Pennsylvania, USA
    J Neurochem 96:118-25. 2006
    ..More importantly, the PSIG activity displays a distinct preference in mediating the 42-site cleavage over the 40-site cleavage, thereby generating Abeta42 as the predominant product...