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Validation and optimization of automated patch-clamp voltage-gated Ca2+ channel assays

Marc Rogers (Metrion CSO) takes part in a collaborative webinar with Nanion Technologies entitled “Validation and optimization of automated patch-clamp voltage-gated Ca2+ channel assays”.

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Cross-site and cross-platform variability of automated patch clamp assessments of drug effects on human cardiac currents in recombinant cells

Kramer, J.; Himmel, H. M.; Lindqvist, A.; Stoelzle-Feix, S.; Chaudhary, K. W.; Li, D.; Bohme, G. A.; Bridgland-Taylor, M.; Hebeisen, S.; Fan, J.; Renganathan, M.; Imredy, J.; Humphries, E. S. A.; Brinkwirth, N.; Strassmaier, T.; Ohtsuki, A.; Danker, T.; Vanoye, C.; Polonchuk, L.; Fermini, B.; Beck Pierson, J.; Gintant, G. Scientific Reports, 2020, 10; 5627

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A systematic strategy for estimating hERG block potency and its implications in a new cardiac safety paradigm

Bradley J. Ridder, Derek J. Leishman, Matthew Bridgland-Taylor, Mohammadreza Samieegohar, Xiaomei Han, Wendy W. Wu, Aaron Randolph, Phu Tran, Jiansong Sheng, Timm Danker, Anders Lindqvist, Daniel Konrad, Simon Hebeisen, Liudmila Polonchuk, Evgenia Gissinger, Muthukrishnan Renganathan, Bryan Koci, Haiyang Wei, Jingsong Fan, Paul Levesque, Jae Kwagh, John Imredy, Jin Zhai, Marc Rogers, Edward Humphries, Robert Kirby, Sonja Stoelzle-Feix, Nina Brinkwirth, Maria Giustina Rotordam, Nadine Becker, Søren Friis, Markus Rapedius, Tom A. Goetze, Tim Strassmaier, George Okeyo, James Kramer, Yuri Kuryshev, Caiyun Wu, Herbert Himmel, Gary R. Mirams, David G. Strauss, Rémi Bardenet, Zhihua Lia. Toxicology and Applied Pharmacology, 394: 114961

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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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Validation of an impedance-based phenotypic screening assay able to detect multiple mechanisms of chronic cardiotoxicity in human stem cell-derived cardiomyocytes

Presentation by Marc Rogers, CSO Metrion Biosciences, Nanion technologies Exhibitor session, 2020 Biophysical Society meeting, San Diego USA.

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