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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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The role of Nav1.7 in human nociceptors: insights from human induced pluripotent stem cell-derived sensory neurons of erythromelalgia patients

Meents, J.E.; Bressan, E.; Sontag, S.; Foerster, A.; Hautvast, P.; Rösseler, C.; Hampl, M.; Schüler, H.; Goetzke, R.; Le TKC.; Kleggetveit, I.P.; Le Cann, K.; Kerth, C.; Rush, A.M.; Rogers, M.; Kohl, Z.; Schmelz, M.; Wagner, W.; Jørum, E.; Namer, B.; Winner, B.; Zenke, M.; Lampert, A. PAIN, March 22, 2019.

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M-type K+ channels in nociceptive pathways: physiological roles and therapeutic potential

Presentation from Metrion Biosciences’ external speaker series, Professor Nikita Gamper, University of Leeds, 5th February 2019.

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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 Activated TEM cells express high levels of the voltage-gated potassium channel Kv1.3, which functions to control cell excitability.

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Assessment of human induced pluripotent stem cell-derived cardiomyocytes for evaluating drug-induced arrhythmias with multi-electrode array

Human induced pluripotent stem cell-derived cardiomyocytes (iPSC-CM) are a promising tool for assessment of drug-induced arrhythmias during non-clinical drug development. This technology is under evaluation by the FDA’s Comprehensive in vitro Proarrhythmia Assay (CiPA) initiative and the Japanese iPS Cardiac Safety Assessment consortium (JiCSA) to develop new cardiac safety assessment measures to refine current S7B and E14 guidelines.

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Poster: New CiPA cardiac ion channel cell lines and assays for in vitro proarrhythmia risk assessment

New cardiac safety testing guidelines are being finalised, as part of the FDA’s Comprehensive in vitro Proarrhythmia Assay (CiPA) initiative, which aim to remove the over-reliance on screening against the hERG channel by expanding the panel to include hNav1.5, hCav1.2, hKv4.3/KChiP2.2, hKir2.1 and hKv7.1/KCNE1 human cardiac ion channels.

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A drug discovery collaboration between Japanese pharma and a UK SME CRO successfully developed novel small molecule inhibitors of the Kv1.3 channel to treat autoimmune disease

The Best of Both Worlds: Innovation, Collaboration and Synergy between CROs and their Customer Partners, Stevenage, 2018

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Recent advances in targeting ion channels to treat chronic pain

Stevens, E.B.; Stephens, G.J. British Journal of Pharmacology. 2018, 175 (12), 2133-2137

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Functional characterisation of human iPSC-derived atrial cardiomyocytes

Atrial fibrillation (AF) is the most common arrhythmia observed in the clinic, considerable effort has been made to identify the cellular mechanisms of AF and develop new safe and effective antiarrhythmic drugs(1). However, preclinical studies using non-cardiac cells and non-human animal models may not replicate the physiology of human atrial cardiomyocytes or predict patient efficacy and safety.

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Utility of human iPSC-derived CMs for preclinical safety assays and disease modelling

This talk was presented by Dr Sarah Williams at the Axol Metrion Interactive Stem Cell Forum held in May 2018. This project received funding from the Eurostars-2 joint program with co-funding from the European Union Horizon 2020 Research and Innovation Program.

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Metrion Biosciences is a contract research organisation (CRO) specialising in high-quality preclinical drug discovery services.
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