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SB Drug Discovery shows the validation of fluorescence and automated electrophysiology assays designed to assess agonists, antagonists and allosteric modulators of these receptors, culminating in a high-throughput electrophysiology assay suited to assessing multiple GABAA receptor subtypes on a single assay plate.
This webinar, held on 25 October 2018, presented the results from integrated fragment-based approaches for Indoleamine 2,3 dioxygenase 1 (IDO1), an enzyme widely recognised as a drug target for the development of immunotherapeutic small molecules in oncology, unveiling the first ligands able to modulate non-catalytic signalling.
Inefficiencies in drug discovery are hard to ignore when despite ever-increasing investment in pharmaceutical research and development, the number of new drugs approved by the US Food and Drug Administration (FDA) remains low.
The relative failure of molecular target-based drug discovery has led to a return to phenotypic screening. Targets that are intracellular necessitate their drug ligands to pass through plasma membranes, where the protein:lipid ratio is often 3:1 by mass and at least 1:1 by area. The widespread view that most of…
Due to the crucial role of G protein-coupled receptors (GPCRs) in mediating cellular responses to external stimuli, these receptors have been and will remain a prime focus for medical research and the pharmaceutical industry for many years to come. Their importance is especially highlighted by the statistic that 30-50% of…
An integrated fragment-based approach, which reveals enzymatic inhibitors with potential therapeutic application, is the subject of this webinar.Taking place on 25 October 2018 at 3:00pm, the webinar is supported by NanoTemper Technologies.
In this application note, we show how the signal of luciferase and fluorophore were acquired simultaneously with the PHERAstar microplate reader...
In this application note we will show how a cAMP BRET biosensor can be used to monitor ligand binding with the help of the CLARIOstar microplate reader...
In this application note, BMG Labtech discuss how the Bioluminescence resonance energy transfer (BRET) is a versatile tool to study interactions and trafficking in proteins.
Researchers have discovered a significant new compound that helps to mobilise a type of T cell – invariant natural killer T (iNKT) cells – in the fight against disease.
Researchers developed an approach and platform to create large amounts of fillable and targeted nanovesicles to deliver drugs to tumours in mice...
15 January 2018 | By BMG Labtech GmbH
Optimising the receptor binding kinetics of new drugs can have significant benefits, ranging from improved duration of action to enhanced efficacy through the insurmountable antagonism of dynamic physiological systems.Despite this, the kinetics of new receptor ligands are rarely measured early in the drug discovery process, largely because current assays are…
Scientists at the Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP) have succeeded in revealing a key mechanism of membrane deformation.
The growth-arrest specific 6 (GAS6) protein has emerged in recent years as an attractive target for drug development primarily because it is the sole ligand for the AXL receptor tyrosine kinase, which plays critical roles in cancer, fibrosis, and viral infection.
A team of scientists from Austria, Australia, Denmark, England and the Czech Republic, led by Christian Gruber from the MedUni Vienna's Institute of Pharmacology, managed to isolate a neuropeptide from ants that is very similar to the human love hormone oxytocin, and the closely related hormone vasopressin.
