Bryan J. Koci

Pharmacological characterization of a primary nicotinic receptor from the neuromuscular junction

Andrew Cook, Muthukrishnan Renganathan, Dazhi Xiong, Cassidy Kilpack et autres

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Optimization of TopoIV Potency, ADMET Properties, and hERG Inhibition of 5-Amino-1,3-dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Identification of a Lead with In Vivo Efficacy against MRSA

Yanran Lu, Sandip M. Vibhute, Linsen Li, Antony A. Okumu et autres

Novel bacterial topoisomerase inhibitors (NBTIs) are among the most promising new antibiotics in preclinical/clinical development. We previously reported dioxane-linked NBTIs with potent antistaphylococcal activity and reduced hERG inhibition, a key safety liability. Herein, polarity-focused optimization enabled the delineation of clear structure–property relationships …

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Formulation, Stability, Pharmacokinetic, and Modeling Studies for Tests of Synergistic Combinations of Orally Available Approved Drugs against Ebola Virus In Vivo

Courtney L. Finch, Julie Dyall, Shuang Bing Xu, Elizabeth A. Nelson et autres

Outbreaks of Ebola ebolavirus (EBOV) have been associated with high morbidity and mortality. Milestones have been reached recently in the management of EBOV disease (EVD) with licensure of an EBOV vaccine and two monoclonal antibody therapies. However, neither vaccines nor therapies are …

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Formulation, Stability, Pharmacokinetic, and Modeling Studies for Tests of Synergistic Combinations of Orally Available Approved Drugs Against Ebola Virus In Vivo

Courtney L. Finch, Julie Dyall, Shuang Bing Xu, Elizabeth A. Nelson et autres

Outbreaks of Ebola ebolavirus (EBOV) have been associated with high morbidity and mortality. Milestones have been reached recently in the management of EBOV disease (EVD) with licensure of an EBOV vaccine and two monoclonal antibody therapies. However, neither vaccines nor therapies are …

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Comparison of 5-HT3 binding and functional activity using the IonFlux™ HT automated patch clamp platform

Jennifer Wesley, Bryan J. Koci, Andrew Cook, Diane Werth

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Functional assessment of hNav1.x ion channels using state-dependent protocols on the QPatch HT automated patch clamp system

Bryan J. Koci, Jennifer Wesley, Muthukrishnan Renganathan, Diane Werth et autres

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Novel bacterial topoisomerase inhibitors derived from isomannide

Antony A. Okumu, Yanran Lu, Sheri Dellos-Nolan, Jonathan L. Papa et autres

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Corrigendum to “A systematic strategy for estimating hERG block potency and its implications in a new cardiac safety paradigm” [Toxicology and Applied Pharmacology volume 394C (2020) 114961]

Bradley J. Ridder, Derek J. Leishman, Matthew H. Bridgland-Taylor, Mohammadreza Samieegohar et autres

© 2020 The Author(s) The authors regret that one affiliation address is mistaken in the published paper. Matthew Bridgland-Taylor's affiliation was incorrectly listed as Clinical Pharmacology & Safety Sciences, R&D, AstraZeneca, Cambridge, United Kingdom. The correct affiliation is Clinical Pharmacology & Safety …

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A systematic strategy for estimating hERG block potency and its implications in a new cardiac safety paradigm

Bradley J. Ridder, Derek J. Leishman, Matthew H. Bridgland-Taylor, Mohammadreza Samieegohar et autres

INTRODUCTION: hERG block potency is widely used to calculate a drug's safety margin against its torsadogenic potential. Previous studies are confounded by use of different patch clamp electrophysiology protocols and a lack of statistical quantification of experimental variability. Since the new cardiac …

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Automated high-throughput Na+ late current assay in QPatch HT platform for CiPA28

Muthukrishnan Renganathan, Bryan J. Koci, Andi Cook, Haiyang Wei et autres

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Optimization of cardiac CiPA targets (hCav1.2 and hKCNQ1/hminK) on the QPatch HT automated system

Bryan J. Koci, Muthukrishnan Renganathan, Andi Cook, Haiyang Wei et autres

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Impedance-Based Assessment of Preclinical Cardiac Structural Toxicity Using Human iPSC-Derived Cardiomyocytes and its Correlation to In Vivo (dog) Exposures

Bryan J. Koci, Greg Luerman, Anika Duenbostell, Ralf Kettenhofen et autres

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