Twelve new peer-reviewed publications using QPatch or Qube 384 in Q3

̶T̶w̶e̶l̶v̶e̶ thirteen new peer-reviewed publications were published in Q3 using QPatch or Qube 384.

Most of the publications this quarter came from the pharma industry, with publications from Gedeon Richter, Eisai, Lundbeck, Sanofi, Novartis, Esteve, Taisho Pharmaceuticals. However, as always, a few from academia with one from University of Heidelberg using Qube 384 and also, as always, a massive input from the University of Queensland with four publications. To our knowledge that brings the University of Queensland up to 12 publications using QPatch in 2020 alone.

NMDA, Cav3.X, the full sodium channel panel Nav1-8 and the entire CiPA safety panel have been investigated. Also, a few of the QPatch publications were only used for hERG safety testing. While this might be of less scientific relevance it is great to see that the QPatch still are the benchmark for cardiac safety testing and hERG counter screens.

Topics are diverse, from NMDA research to early drug discovery and lead optimisation.

Of the more exotic topics, we could highlight Wang er al 2020 and McMahon et al. 2020 using QPatch to characterise the effect of conotoxins, a group of neurotoxic peptides isolated from the venom of the predatory marine cone snails of the genus Conus.

Le Marois et al. 2020 might be a good evening read. This group at Sanofi in Paris, France, has evaluated the effect of the non-psychoactive component of Cannabis (CBD) on seven major cardiac currents. They show that CBD impacts cardiac electrophysiology, so hold back on the cannabis oil if you have heart problems.

Enjoy the read, and remember you can always find QPatch and Qube 384 publications on sophion.com in our publication library

Bozó et al. 2020. “New V1a Receptor Antagonist. Part 2. Identification and Optimization of Triazolobenzazepines.” Bioorganic & Medicinal Chemistry Letters 30(18): 127417.

Fukushima et al. 2020. “Inhibitory Effect of Anti-Seizure Medications on Ionotropic Glutamate Receptors: Special Focus on AMPA Receptor Subunits.” Epilepsy Research 167: 106452.

Grupe et al. 2020. “In Vitro and in Vivo Characterization of Lu AA41178: A Novel, Brain Penetrant, Pan-Selective Kv7 Potassium Channel Opener with Efficacy in Preclinical Models of Epileptic Seizures and Psychiatric Disorders.” European Journal of Pharmacology: 173440.

Le Marois et al. 2020. “Cannabidiol Inhibits Multiple Cardiac Ion Channels and Shortens Ventricular Action Potential Duration in Vitro.” European Journal of Pharmacology 886: 173542.

McMahon et al. 2020. “Discovery, Pharmacological Characterisation and NMR Structure of the Novel µ-Conotoxin SxIIIC, a Potent and Irreversible NaV Channel Inhibitor.” Biomedicines 8(10): 391.

Sharma et al. 2020. “Recombinant Production, Bioconjugation and Membrane Binding Studies of Pn3a , a Selective Na V 1 . 7 Inhibitor.” Biochemical Pharmacology: 114148.

Skepper et al. 2020. “Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria.” Journal of Medicinal Chemistry.

Wang et al. 2020. “Characterisation of δ -Conotoxin TxVIA as a Mammalian T-Type Calcium Channel Modulator.” Marine Drugs 7: 1–13

Peschel et al. 2020. “Two for the Price of One: Heterobivalent Ligand Design Targeting Two Binding Sites on Voltage-Gated Sodium Channels Slows Ligand Dissociation and Enhances Potency.” Journal of Medicinal Chemistry: acs.jmedchem.0c01107

García et al. 2020. “Discovery of EST73502, a Dual μ-Opioid Receptor Agonist and σ 1 Receptor Antagonist Clinical Candidate for the Treatment of Pain.” Journal of Medicinal Chemistry 52862.

Ushiyama et al. 2020. “Lead Optimization of 8-(Methylamino)-2-Oxo-1,2-Dihydroquinolines as Bacterial Type II Topoisomerase Inhibitors.” Bioorganic and Medicinal Chemistry 28(22): 115776.

Merz et al. 2020. “A Microscopy-Based Small Molecule Screen in Primary Neurons Reveals Neuroprotective Properties of the FDA-Approved Anti-Viral Drug Elvitegravir.” Molecular Brain 13(1): 1–14.

Cardoso et al., 2020. “A spider-venom peptide with multitarget activity on sodium and calcium channels alleviates chronic visceral pain in a model of irritable bowel syndrome.” Pain: doi: 10.1097/j.pain.0000000000002041