Cancer - Sophion

Ion Channels and Cancer

Ion channels involved in cancer (click on image to enlarge)

Transport of ions across the cell membranes play a critical role in tumor cell functions, such as cell volume regulation, cell migration, cell cycle progression, cell proliferation and cell death. Functions that are critical for tumor cell survival as well as metastasis.

 

If tumor-relevant ion channels are upregulated by growth factors and hormones to the extent that a given ion channel is critically important for the survival of a tumor cell it might be considered a target for treatment. However, only ion channels applicable to the suppression of tumor growth, which does not serve critically important functions in other cells, (e.g. channels involved in cardiac repolarization) are relevant. Also, potential ion channel targets may be relevant for the proliferation and survival of cells other than tumor cells

Several Ion Channels are currently being investigated as oncogenic or potential targets for anti-cancer drugs.

 

A few examples below:

Rao et Al 2015. Voltage-Gated Ion Channels in Cancer Cell Proliferation (LINK)

Litan and Langhans 2015. Cancer as a channelopathy: ion channels and pumps in tumor development and progression (LINK)

Dowd et Al 2017 Ion Channels in Breast Cancer: From Signaling to Therapy (LINK)

…or check out a search on ion channel and cancer (HERE)

 

See below for QPatch and Qube publications on selected cancer-relevant ion channels

 

Calcium Channels

  • Cav1.2
  • Cav3.2

 

Potassium channels, Calcium activated

  • Kca1.1
  • Kca3.1

 

Potassium channels, voltage-gated

  • Kv1.3
  • Kv1.5
  • Kv11.1 (hERG)

 

Sodium channels, voltage-gated

  • Nav1.5
  • Nav1.7

 

TRP Channels

  • TRPC6
  • TRPM4
  • TRPM8
  • TRPV1
  • TRPV6

 

Calcium activated chloride channel

  • TMEM16A

 


Cav

Posters

  • 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

Papers

  • View The Snake with the Scorpion’s Sting: Novel Three-Finger Toxin Sodium Channel Activators from the Venom of the Long-Glanded Blue Coral Snake
    Year: 2016 First author: Yang et al., 2016

Reports

  • View Cav1.2 on Qube 384
    Year: 2017 First author: Schupp, M

Kca+

Posters

  • View Wnt peptides control mammalian cancer cell membrane potential
    Year: 2018 First author: Ashmore et Al., 2018

Papers

  • View Extracellular K+ Dampens T Cell Functions: Implications for Immune Suppression in the Tumor Microenvironment
    Year: 2019 First author: Ong et Al.
  • View Inhibition of the potassium channel KCa3.1 by senicapoc reverses tactile allodynia in rats with peripheral nerve injury
    Year: 2016 First author: Staala et al., 2016
  • View New positive Ca2+-activated K+ channel gating modulators with selectivity for KCa3.1
    Year: 2014 First author: Coleman et al., 2014
  • 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 Development of a QPatch Automated Electrophysiology Assay for Identifying KCa3.1 Inhibitors and Activators
    Year: 2013 First author: Jenkins et al., 2013

Reports

  • View HEK293-KCa on QPatch
    Year: 2008 First author: Jacobsen et al., 2008
  • View The intermediate conductance Ca2+ – activated K+ channel on Qube 384
    Year: 2017 First author: Sauter

Kv

Posters

  • View Generating potent and selective inhibitors of Kv1.3 ion channels by fusing venom derived mini proteins into peripheral CDR loops of antibodies
    Year: 2019 First author: Karatt-Vellatt et al., 2019
  • View Enhancing throughput with multiple cell lines per well
    Year: 2006 First author: Olsen et al.
  • View Enhancing throughput with multiple cell lines per well with the QPatch HTX
    Year: 2010 First author: Olsen et al., 2010
  • 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
  • Simple and Effective Generation of Cell-based Assays for Ion Channels, Transporters, and Kinase Screening in Biologically Relevant Cells Using Scalable Transient Transfection
    Year: 2014 First author: Chen, Q

Papers

  • View A Novel Modulator of Kv3 Potassium Channels Regulates the Firing of Parvalbumin-Positive Cortical Interneurons
    Year: 2015 First author: Rosata-Siri et al., 2015
  • View A Rational Design of a Selective Inhibitor for Kv1.1 Channels Prevalent in Demyelinated Nerves that Improves their Impaired Axonal Conduction
    Year: 2017 First author: Al-Sabi et al., 2017
  • View Arrangement of Kv1 α subunits dictates sensitivity to tetraethylammonium
    Year: 2010 First author: Al-Sabi et Al
  • View Isoindolinone compounds active as Kv1.5 blockers identified using a multicomponent reaction approach
    Year: 2015 First author: Kajanus et al.
  • View Physiological modulators of Kv3.1 channels adjust firing patterns of auditory brainstem neurons
    Year: 2016 First author: Brown et al., 2016
  • View Porphyrin derivatives as potent and selective blockers of neuronal Kv1 channels
    Year: 2014 First author: Daly et al., 2014
  • View Chemoselective tarantula toxins report voltage activation of wild-type ion channels in live cells
    Year: 2014 First author: Tilleya et al., 2014
  • View Positive allosteric modulators of α7 nicotinic acetylcholine receptors affect neither the function of other ligand- and voltage-gated ion channels and acetylcholinesterase, nor β-amyloid content
    Year: 2016 First author: Ariasa et al., 2016
  • View New positive Ca2+-activated K+ channel gating modulators with selectivity for KCa3.1
    Year: 2014 First author: Coleman et al., 2014
  • 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 Rapid generation of cells for ion channels assays: Efficient, large scale transfection using the MaxCyte STX
    Year: 2012 First author: Brady 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 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 Identification of Selective Inhibitors of the Potassium Channel Kv1.1–1.2(3) by High-Throughput Virtual Screening and Automated Patch Clamp
    Year: 2012 First author: Søren J Wacker 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

Reports

  • View CHO-Kv1.5 Voltage-gated potassium channels on QPatch
    Year: 2009 First author: Jensen et al., 2009
  • View CHO-KvLQT1 minK on QPatch
    Year: 2011 First author: Olsen et al., 2011
  • View High throughput assay for Kv1.5 on Qube 384
    Year: 2020 First author: Daniel Sauter

Nav1.5, Nav1.7

Posters

  • View NaV1.5 big late : An inactivation deficient mutant of NaV1.5 as screening tool for late sodium currents of the cardiac action potential
    Year: 2018 First author: Bouyer et Al.
  • View CHO-hNav1.7 assay on Qube pharmacology, biophysical characterization and the effect of internal fluoride
    Year: 2017 First author: Sauter et al., 2017
  • 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 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 “Clip Detecting” with series resistance compensation using an automated patch clamp system
    Year: 2012 First author: Løjkner et al., 2012
  • View Biophysical and pharmacological characterization of multiple Nav subtypes on Qube
    Year: 2016 First author: Lindqvist et Al
  • View Biophysical and pharmacological profiling of multiple Nav subtypes on QPatch HT
    Year: 2016 First author: Lindqvist et al., 2016

Papers

  • View Co-expression of β Subunits with the Voltage-Gated Sodium Channel NaV1.7: the Importance of Subunit Association and Phosphorylation and Their Effects on Channel Pharmacology and Biophysics
    Year: 2018 First author: Sokolov et Al.
  • View High-Throughput Screening of Nav1.7 Modulators Using a Giga-Seal Automated Patch Clamp Instrument
    Year: 2016 First author: Chambers et al., 2016
  • View Rational engineering defines a molecular switch that is essential for activity of spider-venom peptides against the analgesics target Nav1.7
    Year: 2015 First author: Klint et al., 2015
  • View Engineering Highly Potent and Selective Microproteins Against Nav1.7 Sodium Channel for Treatment of Pain
    Year: 2016 First author: Shcherbatko et al., 2016
  • 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 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 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

Reports

  • 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 Nav1.5(Late) cardiac safety assay on QPatch
    Year: 2019 First author: Edward S A Humphries
  • View CHO-Nav1.5 use-dependent blockers on QPatch
    Year: 2010 First author: M. Knirke Jensen

TRP

Posters

  • View TRP’ing in multi-hole mode
    Year: 2010 First author: Jacobsen et al., 2010

Papers

  • View The development of automated patch clamp assays for canonical transient receptor potential channels TRPC3, 6, and 7
    Year: 2014 First author: McPate et Al.
  • View QPatch: the missing link between HTS and ion channel drug discovery.
    Year: 2009 First author: Mathes
  • View Study of TRP Channels by Automated Patch Clamp Systems
    Year: 2010 First author: Sunesen et al., 2010

Reports

  • View HEK293-TRPV1 on QPatch
    Year: 2011 First author: Jacobsen et al., 2011
  • View TRPM8 cold sensitive ion channels
    Year: 2012 First author: Jensen

TMEM

Papers

  • View Calcium-activated chloride channel ANO1 promotes breast cancer progression by activating EGFR and CAMK signaling
    Year: 2013 First author: Britschgi, A
  • View Development of a QPatch-Automated Electrophysiology Assay for Identifying TMEM16A Small-Molecule Inhibitors
    Year: 2020 First author: Henckels et Al.

Reports

  • View TMEM16A on Qube
    Year: 2017 First author: Sauter, D
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