
QPatch & Qube users have been busy in Q3, publishing 19 more publications
Here are some select highlights:
- Ghovanloo et al., PLoS ONE â 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 â 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 â a thorough examination of cardiac ion channel safety pharmacology in hERG, Cav1.2, and Nav1.5 (peak/late), Dr Steve Jenkinsonâs 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. â more snakebite antivenom antibody (nanobody) discovery & development in the 4th publication arising from a fruitful collaboration between Prof. Andreas Laustsenâs lab at DTU & Sophion application scientist Dr Kim Boddum.
To see publications, click on the links below:
- McMahon et al. (2022). ”-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). StructureâActivity 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)âNâBenzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide [(R)-ASâ1], 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 pharmaâs 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-aÌ-aÌ-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.