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Validation of an ASIC1a ligand-gated assay on an automated patch-clamp platform and it’s use for novel ligand screening

There is growing interest in automated patch-clamp (APC) assays for ligand-gated targets which are expressed throughout the peripheral and central nervous system. The Acid-Sensing Ion Channel (ASIC) family comprises combinations of ASIC1-4 proteins that form acid-activated cation-selective channels.

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Development and validation of ASIC1a ligand-gated ion channel drug discovery assays on automated patch-clamp platforms (Collaboration with Nanion Technologies)

Acid-sensing ion channels (ASICs) are proton-gated ion channels which are highly sensitive to extracellular acidosis and are permeable to cations1, predominantly Na+. To date, six different ASIC subunits (1a, 1b, 2a, 2b, 3 and 4) encoded by four genes have been identified.

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The Nav1.5 late current in WT and Nav1.5 ΔKPQ mutant channels: An automated patch-clamp LQT3 electrophysiological assay

The cardiac late Na+ current (late INa) generates persistent inward currents throughout the plateau phase of the ventricular action potential and is an important determinant of repolarisation rate, EADs and arrythmia risk. As inhibition of late INa can offset drug effects on hERG and other repolarising K+ conductances it is one of the key cardiac channels in the Comprehensive in vitro Proarrythmia Assay CiPA panel being developed by the FDA to improve human clinical arrythmia risk assessment.

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Using new in vitro cardiac ion channel assays and in silico models to predict proarrhythmia risk with automated patch-clamp

The FDA’s Comprehensive in vitro Proarrhythmia Assay (CiPA) initiative is designed to remove the over-reliance on hERG data to predict human clinical cardiac risk, with recent results suggesting that inclusion of additional cardiac ion channels and assays (e.g. peak and late Nav1.5, Cav1.2, dynamic hERG) improve risk predictions of in silico action potential models.

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Identification of novel ion channel binders: TRPA1 antagonist case study (Collaboration with Domainex)

Domainex and Metrion Biosciences have formed an alliance to identify new chemical hits against ion-channel targets. Key to this collaboration are Domainex’s experience in hit identification and Metrion Bioscience’s expertise in ion channel screening and pharmacology.

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Identification of novel scorpion venom peptide inhibitors of the Kv1.3 ion channel and their potential as drug discovery leads for human T-cell mediated disease

Activated effector memory T-cells (TEM) have been implicated in the pathogenesis of autoimmune diseases.1 TEM cells express high levels of the voltage-gated potassium channel, Kv1.3, which plays a role in controlling the function of TEM. Inhibition of Kv1.3 reduces the release of pro-inflammatory mediators, inhibits T-cell proliferation and migration to inflamed tissues, and has been shown to ameliorate autoimmune disease symptoms in preclinical animal models.

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Investigating the correlation between thallium flux and automated patch-clamp for ion channel activators

Ion channels play a key role in regulating resting membrane potential and cell excitability and are attractive targets for therapeutic intervention.

Thallium (Tl+) flux assays, which measure the flow of Tl+ through potassium channels, offer a high throughput method for the identification of potassium channel activators.

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Predicting cardiac proarrhythmic risk exclusively using automated patch-clamp data

Recent work by FDA and HESI CiPA working groups indicate that in vitro hERG, Nav1.5 and Cav1.2 potency data in addition to dynamic hERG kinetic data is required to accurately predict proarrhythmic risk.

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Development of an impedance based screening assay for cardiac safety and cardiotoxicity detection in stem cell derived cardiomyocytes

Cardiac toxicity remains the leading cause of new drug safety side-effects. Current preclinical cardiac safety assays rely on in vitro cell-based ion channel assays and ex vivo and in vivo animal models. These assays provide an indication of acute risk but they do not always predict the effect of chronic compound exposure, as recently seen with oncology drugs.

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Metrion Biosciences: High quality ion channel drug discovery service provider

Metrion Biosciences is a UK based CRO, located at Granta Park in Cambridge. Our team has substantial expertise in providing research services to deliver preclinical and clinical stage drug candidates, and has a proven track record of providing high quality drug discovery services to our customers for ion channel targets on a fee-for-service or collaboration basis. The Metrion team takes pride in providing a knowledgeable, collaborative and flexible service to all customers, whether for small stand alone projects or fully integrated drug discovery programmes.

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