Kun Liu

Summary

Affiliation: Wyeth Research
Country: USA

Publications

  1. doi High-throughput screening for Kv1.3 channel blockers using an improved FLIPR-based membrane-potential assay
    Kun Liu
    Department of Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA
    J Biomol Screen 15:185-95. 2010
  2. doi Rb+ efflux assay for assessment of non-selective cation channel activities
    Kun Liu
    Screening Sciences, Wyeth Research, Collegeville, Pennsylvania, USA
    Assay Drug Dev Technol 8:380-8. 2010
  3. doi 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
  4. doi NPPB structure-specifically activates TRPA1 channels
    Kun Liu
    Department of Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA
    Biochem Pharmacol 80:113-21. 2010
  5. doi Discovery of (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid hydrochloride (GAP-134)13, an orally active small molecule gap-junction modifier for the treatment of atrial fibrillation
    John A Butera
    Chemical Sciences, Wyeth Research, CN 8000, Princeton, New Jersey 08543, USA
    J Med Chem 52:908-11. 2009
  6. doi 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

Collaborators

Detail Information

Publications6

  1. doi High-throughput screening for Kv1.3 channel blockers using an improved FLIPR-based membrane-potential assay
    Kun Liu
    Department of Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA
    J Biomol Screen 15:185-95. 2010
    ..Some compounds possess nanomolar potency, indicating that the FLIPR assay is effective for successfully identifying K(+) channel blockers as novel drug candidates...
  2. doi Rb+ efflux assay for assessment of non-selective cation channel activities
    Kun Liu
    Screening Sciences, Wyeth Research, Collegeville, Pennsylvania, USA
    Assay Drug Dev Technol 8:380-8. 2010
    ..Using this assay for secondary confirmation screen, we successfully identified and confirmed the positive hits as TRPC6 inhibitors...
  3. doi 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...
  4. doi NPPB structure-specifically activates TRPA1 channels
    Kun Liu
    Department of Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA
    Biochem Pharmacol 80:113-21. 2010
    ..None of the single chemical group was sufficient to activate the channel, indicating that NPPB activated TRPA1 through a structure-specific mechanism...
  5. doi Discovery of (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid hydrochloride (GAP-134)13, an orally active small molecule gap-junction modifier for the treatment of atrial fibrillation
    John A Butera
    Chemical Sciences, Wyeth Research, CN 8000, Princeton, New Jersey 08543, USA
    J Med Chem 52:908-11. 2009
    ..Activity of the compounds was confirmed in a mouse cardiac conduction block model of arrhythmia. Dipeptide 9f (GAP-134) was identified as a potent, orally active gap-junction modifier for clinical development...
  6. doi 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...