QPatch & Qube users have been busy in Q3, publishing 19 more publications
Here are some select highlights:
Ghovanloo et al., PLoS ONE – in a collaboration between Simon Fraser University & Xenon Pharmaceuticals, used the Qube to define the effects of cannabidiol on gramicidin currents, & implications for their antibiotic activities.
McMahon et al., Toxins; Wang et al., Membranes – the University of Queensland have two papers. McMahon et al. provide biophysical and pharmacological comparisons of marine snail conotoxins, SxIIIC, SmIIIA & KIIIA, blockers of Nav channels. Wang et al. investigated indole-3-carbinol, a natural product found in Brassica vegetables, their block of T-type calcium channels (Cav3.1-3.3) & roles in cancer anti-proliferation.
Watt et al., JPTM – a thorough examination of cardiac ion channel safety pharmacology in hERG, Cav1.2, and Nav1.5 (peak/late), Dr Steve Jenkinson’s team at Pfizer compared GLP manual patch clamp data, Qube APC & hERG binding data, relating data to compound pro-arrhythmia/Torsades de pointes risk modelling.
Wade et al., Bioconjugate Chem. – more snakebite antivenom antibody (nanobody) discovery & development in the 4th publication arising from a fruitful collaboration between Prof. Andreas Laustsen’s lab at DTU & Sophion application scientist Dr Kim Boddum.
To see publications, click on the links below:
McMahon et al. (2022). µ-Conotoxins Targeting the Human Voltage-Gated Sodium Channel Subtype Nav1.7
Davie et al. (2022). A Potent and Selective Small Molecule Plasma Kallikrein Inhibitor Featuring a Novel P1 Group as a Potential Oral On-Demand Treatment for Hereditary Angioedema.
Toti et al. (2022). Structure−Activity Relationship and Neuroprotective Activity of 1,5-Dihydro-2H-naphtho[1,2-b][1,4]diazepine-2,4(3H)-diones as P2X4 Receptor Antagonists.
Sengupta et al. (2022). Novel benzoxazinone derivative as potent human neutrophil elastase inhibitor: Potential implications in lung injury.
Ghovanloo et al. (2022). Cannabidiol increases gramicidin current in human embryonic kidney cells: An observational study.
Caroff et al. (2022). Design, Synthesis, and Pharmacological Evaluation of Benzimidazolo-thiazoles as Potent CXCR3 Antagonists with Therapeutic Potential in Autoimmune Diseases
Wang et al. (2022). Diindolylmethane Derivatives: New Selective Blockers for T-Type Calcium Channels.
Gu et al. (2022). Targeting the LPA1 signaling pathway for fibrosis therapy: a patent review (2010-present).
Abram et al. (2022). Discovery of (R)‑N‑Benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide [(R)-AS‑1], a Novel Orally Bioavailable EAAT2 Modulator with Druglike Properties and Potent Antiseizure Activity In Vivo.
Meyer et al. (2022). Discovery and In Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the Chemokine Receptor CXCR3 for Autoimmune Diseases.
Watt et al. (2022). Use of high throughput ion channel profiling and statistical modeling to predict off-target arrhythmia risk – One pharma’s experience and perspective.
Jin et al. (2022). Development of fluorine-substituted NH2-biphenyl-diarylpyrimidines as highly potent non-nucleoside reverse transcriptase inhibitors: Boosting the safety and metabolic stability.
Faria et al. (2022). Environmental levels of carbaryl impair zebrafish larvae behaviour: The potential role of ADRA2B and HTR2B.
Wade et al. (2022). Generation of Multivalent Nanobody-Based Proteins with Improved Neutralization of Long α-Neurotoxins from Elapid Snakes. Bioconjugate Chemistry.
Zhang et al. (2022). Structure-Based Optimization of Coumestan Derivatives as Polyketide Synthase 13-Thioesterase(Pks13-TE) Inhibitors with Improved hERG Profiles for Mycobacterium tuberculosis Treatment.
Ma et al. (2022). Use of Solvent Mapping for Characterizing the Binding Site and for Predicting the Inhibition of the Human Ether-á-á-Go-Go-Related K + Channel.
Koester et al. (2022). Discovery of Novel Quinoline-Based Proteasome Inhibitors for Human African Trypanosomiasis (HAT).
Wang et al. (2022). Design, Synthesis, and Biological Evaluation of Androgen Receptor Degrading and Antagonizing Bifunctional Steroidal Analogs for the Treatment of Advanced Prostate Cancer.
Feng et al. (2022). Discovery of Selenium-Containing STING Agonists as Orally Available Antitumor Agents.