Search Results - "Houseman, Kathryn"
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Electrophysiologic characterization of a novel hERG channel activator
Published in Biochemical pharmacology (15-04-2009)“…Activators of the human ether-a-go-go-related gene (hERG) K + channel have been reported recently to enhance hERG current amplitude (five synthetic small…”
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Discovery of novel benzothiazolesulfonamides as potent inhibitors of HIV-1 protease
Published in Bioorganic & medicinal chemistry (03-11-2003)“…The human immunodeficiency virus (HIV) has been shown to be the causative agent for AIDS. The HIV virus encodes for a unique aspartyl protease that is…”
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1,4-Dihydroindeno[1,2-c]pyrazoles with Acetylenic Side Chains as Novel and Potent Multitargeted Receptor Tyrosine Kinase Inhibitors with Low Affinity for the hERG Ion Channel
Published in Journal of medicinal chemistry (03-05-2007)“…The synthesis of a novel series of 1,4-dihydroindeno[1,2-c]pyrazoles with acetylene-type side chains is described. Optimization of those compounds as KDR…”
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Ventricular rate adaptation: A novel, rapid, cellular-based in-vitro assay to identify proarrhythmic and torsadogenic compounds
Published in Journal of pharmacological and toxicological methods (01-07-2011)“…Delayed cardiac repolarization is an established risk factor for proarrhythmia and Torsades-de-Pointes (TdeP) that is typically measured in vitro during slow,…”
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An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists
Published in Bioorganic & medicinal chemistry letters (15-02-2007)“…The optimization of potent MCHr1 antagonist 1 with respect to improving its in vitro profile by replacement of the 3,4-methylenedioxy phenyl (piperonyl) moiety…”
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Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity
Published in Bioorganic & medicinal chemistry letters (15-04-2007)“…A series of potent 2-carboxychromone-based melanin-concentrating hormone receptor 1 (MCHr1) antagonists were synthesized and evaluated for hERG (human…”
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Discovery of a novel class of potent HIV-1 protease inhibitors containing the (R)-(hydroxyethyl)urea isostere
Published in Journal of medicinal chemistry (1993)Get full text
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Characterization of A-935142, a hERG enhancer, in the presence and absence of standard hERG blockers
Published in Life sciences (1973) (20-04-2012)“…In a previous study we found that A-935142 enhanced hERG current in a concentration-dependent manner by facilitating activation, reducing inactivation, and…”
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Drug-Induced hERG Current Enhancement is Modulated by Extracellular Proton and Potassium
Published in Biophysical journal (01-02-2011)Get full text
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Optimization of a Cav1.2 Cell Line for Use on QPatch and PatchXpress
Published in Biophysical journal (01-01-2010)Get full text
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Inhibitors of HIV-1 Protease Containing the Novel and Potent (R)-(Hydroxyethyl)sulfonamide Isostere
Published in Journal of medicinal chemistry (01-02-1995)Get full text
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Optimization of Chromone-2-carboxamide Melanin Concentrating Hormone Receptor 1 Antagonists: Assessment of Potency, Efficacy, and Cardiovascular Safety
Published in Journal of medicinal chemistry (02-11-2006)“…Evaluation of multiple structurally distinct series of melanin concentrating hormone receptor 1 antagonists in an anesthetized rat cardiovascualar assay led to…”
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Ion Channel Toolbox for Cardiac Safety Evaluation
Published in Biophysical journal (01-02-2009)Get full text
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Do hERG Enhancers and Blockers Compete?
Published in Biophysical journal (01-02-2009)Get full text
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Electrophysiologic Characterization of a Complex hERG Channel Activator
Published in Biophysical journal (01-02-2009)Get full text
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The effects of mandated standardized testing on teachers' perceptions on the formation and development of professional learning communities in the schools of the Rock Valley Conference
Published 01-01-2007“…The staff professional development and school improvement model of the professional learning community is a powerful tool for reculturing schools from within…”
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Dissertation -
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New hydroxyethylamine HIV protease inhibitors that suppress viral replication
Published in Journal of medicinal chemistry (01-10-1992)“…The synthesis of analogues of AcSerLeuAsn[Phe-HEA-Pro]IleValOMe (1, JG-365; where HEA stands for the hydroxyethylamine unit 2), a tight-binding inhibitor of…”
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HIV-1 protease inhibitors: ketomethylene isosteres with unusually high affinity compared with hydroxyethylene isostere analogs
Published in Bioorganic & medicinal chemistry (01-09-1994)“…HIV protease is a member of the aspartic proteinase family of proteolytic enzymes which include pepsin and renin. In contrast to the enhanced affinity seen…”
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