26.10.2018

31 new Publications and Reports from Q3

We have been informed that we missed a few publications from the Q3 list we posted some weeks ago. Thanks for letting us know…thats what friends are for.

Here is the (hopefully) complete list of publications from Q3 (and a part of Q2).

Learn more about how cannabis inhibits Nav currents at therapeutically relevant concentrations or venom from the giant red bull ant published by, among others, Xenon Pharmaceuticals, GSK, AstraZeneca, Sanofi, Eisai, Uni Queensland and more

Peer reviewed publications

  • Sokolov et Al 2018. 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. Journal of Molecular Neuroscience (LINK)
  • Kanase et Al 2018. 4-Substituted carbamazepine derivatives: Conformational analysis and sodium channel-blocking properties. Bioorganic & Medicinal Chemistry, Volume 26, Issue 9 (LINK)
  • Gonçalves et Al. 2018. Direct evidence for high affinity blockade of NaV1.6 channel subtype by huwentoxin-IV spider peptide, using multiscale functional approaches. Neuropharmacology, Volume 133, 404-414 (LINK)
  • Zha et Al. 2018. Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. European Journal of Medicinal Chemistry, Volume 148, Pages 140-153 (LINK)
  • Israel et Al. 2018. The E15R Point Mutation in Scorpion Toxin Cn2 Uncouples Its Depressant and Excitatory Activities on Human NaV1.6. J. Med. Chem., 2018, 61 (4), pp 1730–1736 (LINK)
  • Loucif et Al. 2018. GI‐530159, a novel, selective, mechanosensitive two‐pore‐domain potassium (K2P) channel opener, reduces rat dorsal root ganglion neuron excitability. British Journal of Pharmacology (LINK)
  • Xu et Al. 2018. Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect. European Journal of Medicinal Chemistry, Volume 145, Pages 74-85 (LINK)
  • Agwa et Al 2018. Efficient Enzymatic Ligation of Inhibitor Cystine Knot Spider Venom Peptides: Using Sortase A To Form Double-Knottins That Probe Voltage-Gated Sodium Channel NaV7. Bioconjug Chem. 2018 Sep 12. (LINK)
  • Colley et Al 2018. Screening strategies for the discovery of ion channel monoclonal antibodies. Current Protocols in Pharmacology, 82, e44. (LINK)
  • Robinson et Al 2018. A comprehensive portrait of the venom of the giant red bull ant, Myrmecia gulosa, reveals a hyperdiverse hymenopteran toxin gene family. Science Advances 12 Sep 2018:Vol. 4, no. 9 (LINK)
  • Procopiou et Al 2018. Discovery of (S)-3-(3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenyl)-4-((R)-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)butanoic Acid, a Nonpeptidic αvβ6 Integrin Inhibitor for the Inhaled Treatment of Idiopathic Pulmonary Fibrosis. Med. Chem (LINK)
  • Ghovanloo et Al 2018. Inhibitory effects of cannabidiol on voltage-dependent sodium currents. Journal of Biological Chemistry (LINK)
  • Bankar et Al 2018. Selective Nav1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain. (LINK)

Posters

  • Bettini et Al 2018. NMDA Receptor Modulators in QPatch. Evotech Gmbh (LINK)
  • Boddum et Al 2018. Optical modulation of ion channels. Sophion Bioscience. (LINK)
  • Boddum et Al 2018. GABAA receptor pharmacology evaluted in overexpressing HEK cells and primary astrocytes on QPatch. Sophion Bioscience. (LINK)
  • Standing et Al 2018. Development of high-throughput electrophysiological assay for the screening of hERG ion channel modulators using Sophion Qube 384. GlaxoSmithKline (LINK)
  • Klint et Al 2018. HT Automation for patch clamp based primary screen for Nav1.1 using Qube 384. Lundbeck A/S (LINK).
  • Bouyer and Hebeisen 2018. NaV5 big late : An inactivation deficient mutant of NaV1.5 as screening tool for late sodium currents of the cardiac action potential. B’SYS (LINK)
  • Douglin Guo et Al. 2018 Simultaneous measurement of cardiac Nav5 peak and late current in an automated QPatch platform. Pfizer. SPS 2018
  • Koci et Al 2018. Optimization of Cardiac CiPA targets (Cav2 and KCNQ1/MinK) on the QPatch HT automated system. Eurofins. SPS 2018
  • Huphries et Al 2018. New CiPA ion channel cell lines and assays for in vitro proarythmia risk assessment. Metrion Biosciences. SPS 2018. (Will be uploaded soon)
  • Donglin Guo et Al 2018. Simultaneous measurement of cardiac hERG and Nav5 currents using an automated Qube patch clamp platform. Pfizer. SPS 2018. (Will be uploaded soon)
  • Renganathan et Al 2018. Automated High Throughput Na+ Late current Assay on QPatch HT platform for CiPA28. Eurofins. SPS 2018 (Will be uploaded soon)
  • Lindqvist and Christensen 2018. Estimating hERGdrug binding using temperature-controlled high throughput automated patch clamp. Sophion Bioscience. SPS 2018 (Will be uploaded soon)

Application Reports

  • Humphries and Binzer 2018. CiPA hERG Milnes kinetic assay on Qpatch (LINK)
  • Sauter D 2018. Voltage and current clamp recordings of Cor.4U® human iPS cell-derived cardiomyocytes using Sophion’s QPatch (LINK)
  • Boddum K 2018. Ligand gated ion channels: GABAA receptor pharmacology on QPatch (LINK)
  • Sauter D 2018. Human iPS cell-derived cardiomyocytes (Cor.4U®) on Sophion’s Qube 384: voltage and current clamp recordings (LINK)
  • Rosholm & Schupp 2018.2 recordings using QPatch (LINK)
  • Schupp 2018. 8 hours unattended hERG run with ≥97% success rate and consistent pharmacology results (LINK)