Q2 sees a bumper crop of 15 publications using Qube 384 and QPatch

Q2’s bumper crop of papers is a nice mix of industry & academic institutions – see the list of contributing labs below. The 15 publications cover a broad range of ion channels (P2X7, hERG, NMDAR, nicotinic acetyl choline receptors, TRPM5, Kv7.2/7.3) & research (Alzheimer’s, multiple sclerosis, cancer, schizophrenia, amnesia, chronic pain, diabetes, anti-bacterials, epilepsy).

Two of the publications were Sophion authored on cardiac ion channel pharmacology. In collaboration with Toho University, Tokyo, Kazuya Tsurudome, Hironori Ohshiro & Taku Izumi studied the anti-atrial fibrillation drug Oseltamivir. A second publication written by Damian Bell & Bernard Fermini – one of the godfathers of cardiac safety pharmacology – is a wide-ranging review on APC in safety assessment.

Finally, what quarter would be complete without yet more great research emanating from the publishing machine that is the University of Queensland.

In Jiang et al., Glenn King’s lab have published on a tarantula toxin that blocks Nav1.7 ion channels, showing its ability to reduce chronic visceral pain in irritable bowel syndrome (IBS).

Jensen et al., another paper involving the King lab in collaboration with Jennifer Deuis, Irina Vetter & Samuel Robinson’s labs, have done a deep dive into the venomous peptides of the velvet ant.

Congratulations to all labs publishing this quarter including: Yale, Stanford, University of Utah, Lundbeck, Gedeon Richter, Orion Pharma, Boehringer Ingelheim, Peking University, Guizhou University, ESTEVE, Barcelona Institute of Science & Technology, Aptuit, Takeda, Novartis, Linköping University, University of Chinese Academy of Sciences.


The velvet ant (Dasymutilla klugii) – from Jensen et al., U. Queensland


Here you can see all the latest publications:

Kambayashi et al., 2021 Translational Studies on Anti-Atrial Fibrillatory Action of Oseltamivir by its in vivo and in vitro Electropharmacological Analyses

Jensen et al, 2021 Venom chemistry underlying the painful stings of velvet ants (Hymenoptera: Mutillidae)

Hopper et al., 2021 Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139

Bell, D.C. & Fermini, B., 2021 Use of automated patch clamp in cardiac safety assessment: past, present and future perspectives

Li et al., 2021 Identification of poly(ADP-ribose)polymerase 1 and 2 (PARP1/2) as targets of andrographolide using an integrated chemical biology approach

Schuelert et al., 2021 The Glycine Transport Inhibitor Bi 425809 Restores Translatable EEG Deficits in an Acute Mouse Model for Schizophrenia-Related Sensory Processing and Cortical Network Dysfunction

Paradkar et al., 2021 Creation of a new class of radiosensitizers for glioblastoma based on the mibefradil pharmacophore

Ledneczki et al., 2021 HTS-based discovery and optimization of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor

Díaz et al., 2021 Tricyclic Triazoles as σ1Receptor Antagonists for Treating Pain

Barilli et al., 2021 From High-Throughput Screening to Target Validation: Benzo[d]isothiazoles as Potent and Selective Agonists of Human Transient Receptor Potential Cation Channel Subfamily M Member 5 Possessing In Vivo Gastrointestinal Prokinetic Activity in Rodents

Lapointe et al., 2021 Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.

Ottosson et al., 2021 Synthetic resin acid derivatives selectively open the hKV7.2/7.3 channel and prevent epileptic seizures.

Kong et al., 2021 Design, Synthesis, and Biological Evaluation of Novel Pyrimido[4,5-b]indole Derivatives Against Gram-Negative Multidrug-Resistant Pathogens

Jiang et al., 2021 Pharmacological Inhibition of the Voltage-Gated Sodium Channel NaV1.7 Alleviates Chronic Visceral Pain in a Rodent Model of Irritable Bowel Syndrome

Zheng et al., 2021 Discovery of Methylene Thioacetal-Incorporated α-RgIA Analogues as Potent and Stable Antagonists of the Human α9α10 Nicotinic Acetylcholine Receptor for the Treatment of Neuropathic Pain