Ion Channels and Cancer
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
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
Reports
- View Cav1.2 on Qube 384 Year: 2017
Kca+
Posters
- View Wnt peptides control mammalian cancer cell membrane potential Year: 2018
Papers
- View Extracellular K+ Dampens T Cell Functions: Implications for Immune Suppression in the Tumor Microenvironment Year: 2019
- View Inhibition of the potassium channel KCa3.1 by senicapoc reverses tactile allodynia in rats with peripheral nerve injury Year: 2016
- View New positive Ca2+-activated K+ channel gating modulators with selectivity for KCa3.1 Year: 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
- View Development of a QPatch Automated Electrophysiology Assay for Identifying KCa3.1 Inhibitors and Activators Year: 2013
Reports
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
- View Enhancing throughput with multiple cell lines per well Year: 2006
- View Enhancing throughput with multiple cell lines per well with the QPatch HTX Year: 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
- 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
Papers
- View A Novel Modulator of Kv3 Potassium Channels Regulates the Firing of Parvalbumin-Positive Cortical Interneurons Year: 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
- View Arrangement of Kv1 α subunits dictates sensitivity to tetraethylammonium Year: 2010
- View Isoindolinone compounds active as Kv1.5 blockers identified using a multicomponent reaction approach Year: 2015
- View Physiological modulators of Kv3.1 channels adjust firing patterns of auditory brainstem neurons Year: 2016
- View Porphyrin derivatives as potent and selective blockers of neuronal Kv1 channels Year: 2014
- View Chemoselective tarantula toxins report voltage activation of wild-type ion channels in live cells Year: 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
- View New positive Ca2+-activated K+ channel gating modulators with selectivity for KCa3.1 Year: 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
- View Rapid generation of cells for ion channels assays: Efficient, large scale transfection using the MaxCyte STX Year: 2012
- 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
- 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
- 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
Reports
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
- View CHO-hNav1.7 assay on Qube pharmacology, biophysical characterization and the effect of internal fluoride Year: 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
- View Use- and state-dependent Nav1.5 blockers on QPatch X and in vivo and in vitro assays Year: 2010
- View Rapid generation of cells for ion channels assays: Efficient, large scale transfection using the MaxCyte STX Year: 2012
- View Enhancing throughput with multiple cell lines per well Year: 2006
- View “Clip Detecting” with series resistance compensation using an automated patch clamp system Year: 2012
- View Biophysical and pharmacological characterization of multiple Nav subtypes on Qube Year: 2016
- View Biophysical and pharmacological profiling of multiple Nav subtypes on QPatch HT Year: 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
- View High-Throughput Screening of Nav1.7 Modulators Using a Giga-Seal Automated Patch Clamp Instrument Year: 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
- View Engineering Highly Potent and Selective Microproteins Against Nav1.7 Sodium Channel for Treatment of Pain Year: 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
- View Use- and state-dependent Nav1.5 blockers on QPatch X and in vivo and in vitro assays Year: 2010
- View MICE Models: Superior to the HERG Model in Predicting Torsade de Pointes Year: 2013
- View A new classifier-based strategy for in-silico ion-channel cardiac drug safety assessment Year: 2015
- View Screening system for drug-induced arrhythmogenic risk combining a patch clamp and heart simulator Year: 2015
Reports
TRP
Posters
- View TRP’ing in multi-hole mode Year: 2010
Papers
Reports
TMEM
Papers
Reports
- View TMEM16A on Qube Year: 2017