GPCRs

Hit discovery for GPCRs: HTS or virtual screens?

8 April 2021 | By Beacon Discovery

Watch our on-demand webinar and learn from an industry expert regarding GPCR virtual screening approaches and challenges and much more.

Anti-C5aR antibody shows promise as immuno-oncology treatment

12 November 2020 | By Victoria Rees (Drug Target Review)

Pre-clinical studies have shown that the TJ210/MOR210 monoclonal antibody is successful at targeting tumours.

Could GPCRs be causing people to respond differently to the same drug?

16 October 2020 | By Hannah Balfour (Drug Target Review)

Hannah Balfour explores how genetic variation in G-protein-coupled receptors (GPCRs) and the proteins that regulate the duration of G protein signalling could be contributing to disease and people’s divergent responses to the same therapeutics.

Cell-based Surface Plasmon Resonance with AstraZeneca

4 June 2020 | By Biosensing Instrument

In this webinar, we will provide an overview of the technology with some application examples and also see a case study how AstraZeneca is exploring SPRM for studies on G-protein-coupled receptors (GPCR) in close collaboration with Biosensing Instrument.

Dynamics of GPCRs revealed using combination of approaches

26 May 2020 | By Hannah Balfour (Drug Target Review)

A team used both structural and spectroscopic techniques to study the dynamics of cell surface G-protein coupled receptors (GPCRs).

Expert view: The path to the high-hanging fruit: access to greater diversity and rapid down-selection

24 March 2020 | By Berkeley Lights

Therapeutic monoclonal antibodies are proven and effective treatment options but many of the ‘low-hanging fruit’ therapeutics have already been identified.

Computational method enhances drug target stability

1 April 2019 | By Drug Target Review

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...

New frontiers in G protein-coupled receptor drug discovery

10 December 2018 | By Christopher J. Langmead

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.

Frizzled receptors could be drug targets for treating major diseases

5 December 2018 | By Iqra Farooq (Drug Target Review)

Frizzled receptors, from the GPCR family, could soon be a target to treat numerous diseases such as cancer, fibrosis and CVD...

Drug Target Review – Issue 4 2018

26 November 2018 | By Drug Target Review

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.

Application note: Cellular dopamine and intracellular calcium signaling using the next generation HTS microplate reader

16 November 2018 | By BMG Labtech GmbH

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.

Application note: NanoBRET^TM assay for monitoring of ligand binding to GPCRs in live cells, using the CLARIOstar^® and the PHERAstar^® FS

17 September 2018 | By BMG Labtech GmbH

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…

Expert view: Managing the complexity of finding new targets and drugging the undruggable

5 September 2018 | By Steven G Jarvis (Head of Pharma & Biotech Segment Strategy - MilliporeSigma)

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.

SB Drug Discovery Ltd

Application note: Monitoring receptor ligand binding in living cells

8 August 2018 | By Dominik Schelshorn (Geneva Biotech), Franka Maurer (BMG Labtech)

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...