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20 February 2017 | By BMG Labtech GmbH
Due to their role in signal transmission from the outside to the inside of a cell, G-protein coupled receptors (GPCRs) are prominent drug targets.
21 October 2016 | By DiscoverX Corporation
Monitoring cellular drug penetration and drug-target interaction enables assessment of compound efficacy and confirmation of mode of action...
3 October 2016 | By Cisbio Bioassays
Cisbio Bioassays has supported GPCR investigation for many years regularly creating cutting edge assays and technologies suited to receptor characterization, compound screening and lead optimization...
In vitro high-throughput cellular target-based assays are commonly used for hit identification targeting G-protein coupled receptors (GPCR). Agonist and antagonist identification of GPCRs often relies on the screening of large collections of chemicals using miniaturised in vitro cell-based functional assays. In the panel of assays, calcium mobilisation measured by aequorin…
29 June 2016 | By Victoria White, Digital Content Producer
Heptares Therapeutics and leadXpro are to employ powerful new approaches for the determination of high-resolution X-ray structures of GPCRs...
18 April 2016 | By Victoria White, Digital Content Producer
Heptares and Kymab are to colllaborate to discover, develop and commercialise novel antibody therapeutics targeting a number of GPCRs...
22 February 2016 | By DiscoverX Corporation
GPCRscan is a functional cell-based GPCR assay panel for profiling drug compounds during drug discovery...
30 November 2015 | By Victoria White
Heptares and Pfizer have announced they are to research and develop potential new medicines directed at up to 10 G protein-coupled receptor (GPCR) targets across multiple therapeutic areas...
The large family of pharmaceutical targets represented by G-protein coupled receptors (GPCRs) are usually involved in a number of intracellular effector pathways, leading to many cellular outcomes. In recent years it has been uncovered that different ligands of a given GPCR may engage the pathways selectively, in that ligands that…
Although this target class is already heavily investigated, there are still a significant number of opportunities for discovery of novel drugs targeting additional GPCRs. In this review, scientists from AstraZeneca R&D discuss the general build-up of GPCR screening cascades for discovery of chemical leads that can be further developed into…
Chemokines orchestrate leukocyte trafficking in the immune system, but unregulated or inappropriate chemokine activity plays a key role in many inflammatory, allergic and autoimmune diseases as well as metastatic tumour progression. The chemokine network is comprised of ~50 distinct ligands that specifically bind and activate a family of 20 G…
