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The benefits of targeting ion channels for pain and some of the hurdles in developing successful ion channel modulators

As part of the the LabTube meets series of interviews Marc Rogers, Metrion Biosciences CSO, outlines the benefits of targeting ion channels for pain and some of the hurdles in developing successful ion channel modulators.

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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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Ion channel drug discovery and modern medicine

Rogers, M. MedNous, November-December 2019. Article published in the November-December 2019 edition of ‘MedNous’, a publication of Evernow Publishing Ltd.

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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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The development of a set of novel small molecule inhibitors of the Kv1.3 ion channel

Ion channels represent 15 – 20% of historic drug approvals and recent drug discovery projects. Many ion channel families (Nav, Cav, TRPx and GABA) are validated as therapeutic targets based on human genetics, animal models and selective pharmacology. However, ion channels are challenging targets requiring expert target class knowledge and specialised screening technology such as automated patch-clamp (APC) electrophysiology.

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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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