Cardiovascular - Sophion

Cardiac Ion Channels

The cardiac action potential is the output of multiple ion channels. The cardiac ion channels are a target for cardiac channelopathies often referred to as long QT syndrome (LQTS), but also an important part of any cardiac safety assessment in drugs.

 

Below see selected publications, posters and reports on various ion channel targets performed on QPatch or Qube.

 

Key Cardiac Ion Channels

Kv11.1 (hERG)

Nav1.5

Cav1.2

Kv7.1 (KvLQT/MinK)

Kv4.3

Kv1.5


Kv11.1 (hERG)

Posters

  • View Estimating hERG drug binding using temperature-controlled high throughput automated patch clamp
    Year: 2018 First author: Lindqvist et al.
  • View Development of high-throughput electrophysiological assay for the screening of hERG ion channel modulators using Sophion Qube 384
    Year: 2018 First author: Standing et Al.
  • View Are stem-cell cardiomyocytes a viable cellular reagent for automated patch-clamp?
    Year: 2017 First author: Morton
  • View Temperature effect on hERG channel pharmacology measured using the Qube automated patch clamp system
    Year: 2017 First author: Lindqvist
  • View Qube as a tool for assay optimization of CiPA cells and protocols by using multiple IC, EC solutions and hERG, Nav1.5 and Cav1.2 on the same QChip
    Year: 2016 First author: Schupp et al., 2016
  • View Enhancing throughput with multiple cell lines per well
    Year: 2006 First author: Olsen et al.
  • View Characterization of hERG blockers using the automated QPatch 16 screening system
    Year: 2005 First author: Jacobsen et al., 2005
  • View Data quality is not affected by cell suspension density
    Year: 2006 First author: Mathes et al., 2006
  • View Strategies for enhancing throughput in ion channel drug screening
    Year: 2008 First author: Jacobsen et al., 2008
  • View Pharmacological characterization of voltage- and ligand-gated ion channels
    Year: 2006 First author: Olsen et al., 2006
  • View “Clip Detecting” with series resistance compensation using an automated patch clamp system
    Year: 2012 First author: Løjkner et al., 2012
  • View Optimizing CHO hERG for automated patch clamping
    Year: 2006 First author: Friis et al., 2006
  • View Verification of CiPA Recommended Voltage Protocols in Patch-Clamp Assay for hERG, Cav1.2 and Late Nav1.5 Currents
    Year: 2019 First author: Katayama et Al., 2019

Papers

  • View MICE Models: Superior to the HERG Model in Predicting Torsade de Pointes
    Year: 2013 First author: Kramer et al., 2013
  • View Cardiomyocytes Derived from Human Induced Pluripotent Stem Cells: An In-Vitro Model to Predict Cardiac Effects of Drugs
    Year: 2017 First author: Sube
  • View Discovery and electrophysiological characterization of SKF-32802; a novel hERG agonist found through a large-scale structural similarity search
    Year: 2017 First author: Donovan, Brian T. et Al.
  • View A dipolar cycloaddition reaction to access 6-methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines enables the discovery synthesis and preclinical profiling of a P2X7 antagonist clinical candidate
    Year: 2017 First author: Chrovian et Al.
  • View Synthesis and biological evaluation of novel 6,11-dihydro-5H-benzo[e]pyrimido- [5,4-b][1,4]diazepine derivatives as potential c-Met inhibitors
    Year: 2017 First author: Huang
  • View Characterization of Potassium Channel Modulators with QPatch™ Automated Patch-Clamp Technology: System Characteristics and Performance To cite this article:
    Year: 2004 First author: Kutchinsky et al., 2004
  • View Cross-site and cross-platform variability of automated patch clamp assessments of drug effects on human cardiac currents in recombinant cells
    Year: 2020 First author: Kramer et Al.
  • View Automated Patch Clamping Using the QPatch
    Year: 2009 First author: Jones et al. 2009
  • View Automated Planar Electrode Electrophysiology in Drug Discovery: Examples of the Use of QPatch in Basic Characterization and High Content Screening on Nav, KCa2.3, and Kv11.1 Channels
    Year: 2009 First author: Korsgaard et al., 2009
  • View QPatch: the missing link between HTS and ion channel drug discovery.
    Year: 2009 First author: Mathes
  • View A new classifier-based strategy for in-silico ion-channel cardiac drug safety assessment
    Year: 2015 First author: Mistry et al., 2015
  • View Screening system for drug-induced arrhythmogenic risk combining a patch clamp and heart simulator
    Year: 2015 First author: Okada et al., 2015
  • View Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel
    Year: 2018 First author: Haile et Al., 2018
  • View Easy-To-Synthesize Spirocyclic Compounds Possess Remarkable in Vivo Activity against Mycobacterium tuberculosis
    Year: 2018 First author: Guardia et Al., 2018
  • View A systematic strategy for estimating hERG block potency and its implications in a new cardiac safety paradigm
    Year: 2020 First author: Ridder et Al.
  • View Bumped Kinase Inhibitors as therapy for apicomplexan parasitic diseases: lessons learned
    Year: 2020 First author: Choi et Al.
  • View Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs
    Year: 2020 First author: Katavolos et Al.
  • View Drug-induced QT prolongation: Concordance of preclinical anesthetized canine model in relation to published clinical observations for ten CiPA drugs
    Year: 2020 First author: Koshman et Al.
  • View Novel Indirect AMP-Activated Protein Kinase Activators: Identification of a Second-Generation Clinical Candidate with Improved Physicochemical Properties and Reduced hERG Inhibitory Activity
    Year: 2020 First author: Kuramoto et Al.
  • View Privileged scaffold-based design to identify a novel drug-like 5-HT7 receptor-preferring agonist to target Fragile X syndrome
    Year: 2020 First author: Lacivita et Al.
  • View Design, synthesis and biological activity of novel 2,3,4,5-tetra-substituted thiophene derivatives as PI3Kα inhibitors with potent antitumor activity
    Year: 2020 First author: Liao et Al.
  • View Novel bacterial topoisomerase inhibitors derived from isomannide
    Year: 2020 First author: Okumu et Al.
  • View EST64454: a Highly Soluble σ 1 Receptor Antagonist Clinical Candidate for Pain Management
    Year: 2020 First author: Diaz et al., 2020
  • View Discovery and characterization of ORM‐11372, a novel inhibitor of the sodium‐calcium exchanger with positive inotropic activity
    Year: 2020 First author: Otsomaa et al., 2020
  • View Discovery of EST73502, a Dual μ-Opioid Receptor Agonist and σ1 Receptor Antagonist Clinical Candidate for the Treatment of Pain
    Year: 2020 First author: Garcia et Al.
  • View Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties
    Year: 2020 First author: Soth et al., 2020
  • View Lead optimization of 2-hydroxymethyl imidazoles as non-hydroxamate LpxC inhibitors: Discovery of TP0586532
    Year: 2020 First author: Ushiyama et al., 2020

Reports

  • View Nav1.5(Late) cardiac safety assay on QPatch
    Year: 2019 First author: Edward S A Humphries
  • View CiPA hERG Milnes kinetic assay on QPatch
    Year: 2018 First author: Humphries et al.
  • View 8 hours unattended hERG run with ≥97% success rate and consistent pharmacology results
    Year: 2018 First author: Schupp et Al.
  • View CHO-hERG Duo characterization and functional validation on QPatch
    Year: 2011 First author: Jacobsen et al., 2011
  • View CHO-hERG Duo in multi-hole mode on QPatch
    Year: 2011 First author: Jacobsen et al., 2011
  • View Stable response for ligand and voltage-gated ion channels on QPatch
    Year: 2010 First author: Olsen et al., 2010
  • View Temperature control on Qube 384 – pharmacological dependency of hERG reference compounds
    Year: 2017 First author: R Jacobsen
  • View hiPSC-derived cardiomyocyte recordings using physiological solutions on QPatch II
    Year: 2021 First author: Rosholm et al.
  • View hERG compound screening at 22°C and 35°C on QPatch II
    Year: 2022 First author: Badone et al.

Nav1.5

Posters

  • View Biophysical and pharmacological profiling of multiple voltage-gated sodium channel subtypes on QPatch II
    Year: 2019 First author: Sauter et Al.
  • View Qube as a tool for assay optimization of CiPA cells and protocols by using multiple IC, EC solutions and hERG, Nav1.5 and Cav1.2 on the same QChip
    Year: 2016 First author: Schupp et al., 2016
  • View Biophysical and pharmacological characterization of multiple Nav subtypes on Qube
    Year: 2016 First author: Lindqvist et Al
  • View Electrophysiological properties of iCell cardiomyocytes obtained by automated patch clamp
    Year: 2011 First author: Schrøder et al., 2011
  • View Use- and state-dependent Nav1.5 blockers on QPatch X and in vivo and in vitro assays
    Year: 2010 First author: Jensen et al.
  • View Rapid generation of cells for ion channels assays: Efficient, large scale transfection using the MaxCyte STX
    Year: 2012 First author: Brady et al.
  • View Enhancing throughput with multiple cell lines per well
    Year: 2006 First author: Olsen et al.
  • View Verification of CiPA Recommended Voltage Protocols in Patch-Clamp Assay for hERG, Cav1.2 and Late Nav1.5 Currents
    Year: 2019 First author: Katayama et Al., 2019
  • View Are stem-cell cardiomyocytes a viable cellular reagent for automated patch-clamp?
    Year: 2017 First author: Morton
  • View Hesperetin preferentially inhibits slow-activating currents of an LQT3 syndrome Na+ channel mutation
    Year: 2018 First author: Alvarez-Collazo et Al., 2018
  • View Biophysical and pharmacological profiling of multiple Nav subtypes on QPatch HT
    Year: 2016 First author: Lindqvist et al., 2016
  • View Adaptive voltage control ensures the precise half inactivation application of voltage-gated channels on automated patch clamp system
    Year: 2019 First author: Tsurudome et Al.

Papers

  • View Cross-site and cross-platform variability of automated patch clamp assessments of drug effects on human cardiac currents in recombinant cells
    Year: 2020 First author: Kramer et Al.
  • View Cardiac sodium channel antagonism – Translation of preclinical in vitro assays to clinical QRS prolongation
    Year: 2017 First author: Jenkinson, S.
  • View Use- and state-dependent Nav1.5 blockers on QPatch X and in vivo and in vitro assays
    Year: 2010 First author: Jensen et al.
  • View Automated Planar Electrode Electrophysiology in Drug Discovery: Examples of the Use of QPatch in Basic Characterization and High Content Screening on Nav, KCa2.3, and Kv11.1 Channels
    Year: 2009 First author: Korsgaard et al., 2009
  • View MICE Models: Superior to the HERG Model in Predicting Torsade de Pointes
    Year: 2013 First author: Kramer et al., 2013
  • View A new classifier-based strategy for in-silico ion-channel cardiac drug safety assessment
    Year: 2015 First author: Mistry et al., 2015
  • View Screening system for drug-induced arrhythmogenic risk combining a patch clamp and heart simulator
    Year: 2015 First author: Okada et al., 2015
  • View Simultaneous assessment of compound activity on cardiac Nav1.5 peak and late currents in an automated patch clamp platform
    Year: 2019 First author: Guo et Al.

Reports

  • View Nav1.5(Late) cardiac safety assay on QPatch
    Year: 2019 First author: Edward S A Humphries
  • View CHO-Nav1.5 on QPatch
    Year: 2012 First author: Olsen
  • View Use- and state-dependent Nav1.5 blockers on QPatch X and in vivo and in vitro assays
    Year: 2010 First author: Jensen et al.
  • View CHO-Nav1.5 use-dependent blockers on QPatch
    Year: 2010 First author: M. Knirke Jensen
  • View hiPSC-derived cardiomyocytes – Nav1.5 compound screening on QPatch® II
    Year: 2022 First author: Beatrice Badone, Stefania Karatsiompani

Cav1.2

Posters

  • View Verification of CiPA Recommended Voltage Protocols in Patch-Clamp Assay for hERG, Cav1.2 and Late Nav1.5 Currents
    Year: 2019 First author: Katayama et Al., 2019
  • View Qube as a tool for assay optimization of CiPA cells and protocols by using multiple IC, EC solutions and hERG, Nav1.5 and Cav1.2 on the same QChip
    Year: 2016 First author: Schupp et al., 2016
  • View Exploring stem cell-derived cardiomyocytes with automated patch clamp techniques
    Year: 2012 First author: Schrøder et al., 2012
  • View Are stem-cell cardiomyocytes a viable cellular reagent for automated patch-clamp?
    Year: 2017 First author: Morton

Papers

  • View Cross-site and cross-platform variability of automated patch clamp assessments of drug effects on human cardiac currents in recombinant cells
    Year: 2020 First author: Kramer et Al.
  • View Cardiac safety assessment with motion field imaging analysis of human iPS cell-derived cardiomyocytes is improved by an integrated evaluation with cardiac ion channel profiling
    Year: 2019 First author: Isobe et Al.
  • View A new classifier-based strategy for in-silico ion-channel cardiac drug safety assessment
    Year: 2015 First author: Mistry et al., 2015
  • View Screening system for drug-induced arrhythmogenic risk combining a patch clamp and heart simulator
    Year: 2015 First author: Okada et al., 2015
  • View MICE Models: Superior to the HERG Model in Predicting Torsade de Pointes
    Year: 2013 First author: Kramer et al., 2013
  • View A big Molecule Induces Schwann cells in the peripheral nervous system leading to Myelin Sheath Repair
    Year: 2020 First author: Rozenfeld et Al.
  • View Use of high throughput ion channel profiling and statistical modeling to predict off-target arrhythmia risk – One pharma’s experience and perspective
    Year: 2022 First author: Watt et al.

Reports

  • View hCav1.2 recordings on Qube 384 using step, train and CiPA protocols
    Year: 2018 First author: Schupp
  • View hCav1.2 recordings using QPatch
    Year: 2018 First author: Rosholm et Al.
  • View Cav1.2 on Qube 384
    Year: 2017 First author: Schupp, M
  • View Cav1.2 on Qube 384 – pharmacology, stability and CiPA
    Year: 2018 First author: Schupp et Al., 2018
  • View Keep it simple – Ready-To-Use Cav1.2 cells on Qube 384
    Year: 2020 First author: Schupp

Kv7.1 (KvLQT/MinK)

Posters

  • View Enhancing throughput with multiple cell lines per well
    Year: 2006 First author: Olsen et al.
  • View Automation of patch clamp techniques: Technical validation through characterization of voltage-gated potassium channels and ligand-gated ion channels
    Year: 2004 First author: Krywkowski et al., 2004

Papers

  • View Cell volume and membrane stretch independently control K+ channel activity
    Year: 2009 First author: Hammami et al., 2009

Reports

  • View CHO-KvLQT1 minK on QPatch
    Year: 2011 First author: Olsen et al., 2011

Kv4.3

Posters

  • View A pharmacological synopsis of small molecules, toxins and CiPA compounds targeting human cardiac Kv4.3 channels
    Year: 2019 First author: Schombert et Al., 2019

Papers

  • View Screening system for drug-induced arrhythmogenic risk combining a patch clamp and heart simulator
    Year: 2015 First author: Okada et al., 2015

Kv1.5

Posters

  • View Enhancing throughput with multiple cell lines per well
    Year: 2006 First author: Olsen et al.
  • View Pharmacological characterization of voltage- and ligand-gated ion channels
    Year: 2006 First author: Olsen et al., 2006

Papers

  • View Isoindolinone compounds active as Kv1.5 blockers identified using a multicomponent reaction approach
    Year: 2015 First author: Kajanus et al.

Handouts

  • View CHO-Kv1.5 Voltage-gated potassium channels on QPatch
    Year: 2009 First author: Jensen et al., 2009
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