10 toasty-fresh-off-the-press publications were published in Q1 using QPatch or Qube 384.

2021 is off to a flying start with 10 QPatch or Qube 384 publications.

Unsurprisingly, the ion channel community have turned their attention to Covid-19 research. Three papers this quarter (from collaborations between UCB, B’SYS GmbH, Charles River Laboratories, Eli Lilly and Company, Certara, University of Oxford, Eisai, University of Tokyo, Novartis & AnaBios Corporation) studied the cardiac ion channel safety of the anti-malarials chloroquine & hydroxychloroquine, that were proposed as re-purposed Covid-19 medications.

A further 7 publications were evenly split between pharma (Novartis, Orion Pharma, Gedeon Richter, Tsumura & Co.) & academic research (University of Queensland; Flinders University; SAHMRI; University of Pittsburgh; Kyushu Dental University; University of Dundee; Infectious Disease Research Institute, Seattle). They cover a veritable cornucopia of ion channel science: pain, irritable bowel syndrome, tuberculosis, cognitive enhancement & safety pharmacology assessment.

Two selected highlights from this quarter’s publications:

Cardoso et al. & Hasan et al. – not one but two more publications off the red-hot printing press at the University of Queensland. In the first, Cardoso et al. describe tarantula toxin activity on ion channels in chronic visceral pain. The second, Hasan et al. compared transient transfection methods for CaV2.2 & NaV1.7 ion channel expression, using QPatch to define the channels’ biophysics & pharmacology. This excellent methods paper will be presented at our next virtual Sophion User Meeting by Drs. Mahadhi Hasan & Fernanda Cardoso on 6th May. Read more here.

Enjoy this quarter’s reading list and don’t forget: you can always find QPatch and Qube 384 publications on sophion.com in our Publication library

Markert et al., 2021 “Discovery of LYS006, a Potent and Highly Selective Inhibitor of Leukotriene A 4 Hydrolase. Journal of Medicinal Chemistry, 64(4), 1889–1903.

Delaunois et al., 2021 Applying the CiPA Approach to Evaluate Cardiac Proarrhythmia Risk of some Antimalarials Used Off-label in the First Wave of COVID-19. European Journal of Medicinal Chemistry.

Okada et al., 2021 “Chloroquine and hydroxychloroquine provoke arrhythmias at concentrations higher than those clinically used to treat COVID-19. A simulation study”. Clinical and Translational Science.

Hasan et al., 2021 “Transfection methods for high-throughput cellular assays of voltage-gated calcium and sodium channels involved in pain”. PLOS ONE, 16(3), e0243645.

Jordaan et al., 2021 “Cardiotoxic Potential of Hydroxychloroquine, Chloroquine and Azithromycin in Adult Human Primary Cardiomyocytes”. Toxicological Sciences.

Ray et al., 2021 “Spirocycle MmpL3 Inhibitors with Improved hERG and Cytotoxicity Profiles as Inhibitors of Mycobacterium tuberculosis Growth”. ACS Omega.

Borgini et al., 2021 “Chemical modulation of Kv7 potassium channels”. RSC Medicinal Chemistry.

Ledneczki et al., 2021 “Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach”. European Journal of Medicinal Chemistry, 214, 113189.

Miyamura et al., 2021 “Isoliquiritigenin, an active ingredient of Glycyrrhiza, elicits antinociceptive effects via inhibition of Nav channels”. Naunyn-Schmiedeberg’s Archives of Pharmacology.

Cardoso et al., 2021 “A spider-venom peptide with multitarget activity on sodium and calcium channels alleviate chronic visceral pain in a model of irritable bowel syndrome”. Pain, 162(2), 569–581.