List view / Grid view

GPCRs

 

New frontiers in G protein-coupled receptor drug discovery

10 December 2018 | By

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.

Drug Target Review – Issue 4 2018

26 November 2018 | By

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: NanoBRETTM assay for monitoring of ligand binding to GPCRs in live cells, using the CLARIOstar® and the PHERAstar® FS

17 September 2018 | By

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

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.