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Dynamics of GPCRs revealed using combination of approaches
A team used both structural and spectroscopic techniques to study the dynamics of cell surface G-protein coupled receptors (GPCRs).
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GPCRs
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Expert view: The path to the high-hanging fruit: access to greater diversity and rapid down-selection
Therapeutic monoclonal antibodies are proven and effective treatment options but many of the ‘low-hanging fruit’ therapeutics have already been identified.
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Computational method enhances drug target stability
Scientists have developed a new computational method for the design of thermally stable G protein-coupled receptors (GPCRs) that are of great help in creating new drugs...
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New frontiers in G protein-coupled receptor drug discovery
G protein-coupled receptors (GPCRs) are seven transmembrane spanning proteins that mediate the physiological responses to a broad array of stimuli, including photons, biogenic amines, peptides and large proteins. They represent the target of approximately one-third of all approved drugs,1 yet paradoxically remain a relatively under-exploited protein class.
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Frizzled receptors could be drug targets for treating major diseases
Frizzled receptors, from the GPCR family, could soon be a target to treat numerous diseases such as cancer, fibrosis and CVD...
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Drug Target Review – Issue 4 2018
In this issue: Omics-informed drug target discovery in combating emerging infectious diseases, measuring intracellular ATP levels to access compound-mediated cellular toxicity, and turning organoids into physiologically relevant high-content assays for drug discovery.
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Application note: Cellular dopamine and intracellular calcium signaling using the next generation HTS microplate reader
This application note highlights the direct optic bottom reading performance of the BMG LABTECH microplate readers in two different cell-based fluorescence intensity assays from Invitrogen.
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Application note: NanoBRETTM assay for monitoring of ligand binding to GPCRs in live cells, using the CLARIOstar® and the PHERAstar® FS
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…
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Expert view: Managing the complexity of finding new targets and drugging the undruggable
Assessing targets that are unable – or rather, extremely difficult – to reach pharmacologically, has prevented researchers from achieving desired clinical successes, most notably in the realm of cancer research. However, many advances are being made to shedlight on these difficult yet desirable target areas.
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Application note: Monitoring receptor ligand binding in living cells
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...
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Application note: Real-time detection of Gs and Gi Signalling in living cells
Genetically-encoded biosensors from Montana Molecular allow for detection of GPCR signalling...
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Application note: CRISPR/Cas9 genome-edited cells express nanoBRET-donor that monitors protein interaction and trafficking
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.
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Study changes long-held concepts of cell decoding
NIH scientists discover macromolecular complexes that could enable medication development...
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Application note: Simultaneous detection of GPCR second messengers in living cells
Due to their role in signal transmission from the outside to the inside of a cell, G-protein coupled receptors are prominent drug targets...