G protein coupled receptors (GPCRs) are essential drug targets for therapeutic intervention due to their integral roles in a plethora of fundamental signal transduction pathways. Indeed, GPCRs ...

GPCRs constitute the largest class of known targets in commercial drug discovery today—collectively the targets of at least 30% of currently marketed drugs. Yet, as heptahelical transmembrane ...

GPCR-targeting drugs make up around a third of those approved by the FDA, yet often come with side effects. New research into the mechanisms of GPCR activation could help design drugs to prevent side ...

However, the market also faces several challenges, including the inherent complexity of GPCR signaling pathways, the risk of off-target effects, and the difficulty of achieving functional selectivity.

These many types of GPCR have one feature in common that makes them particularly difficult to study: when they are activated (whether by a beam of light or a blood-borne hormone), they set off a rapid ...

Adverse side effects ensue if drugs acting on GPCRs activate multiple signaling pathways rather than a specific target pathway.

Since input arrives at the cell exterior and initiates signalling pathways inside the cell, this makes GPCRs useful in pharmacology as the drug in many cases need not enter the cell.

The second pathway is mediated by a completely different G protein-coupled set of cellular receptors (GPCRs). Both classes of receptors deliver molecular messages from outside to inside the cell ...

Duke University Medical Center researchers have discovered that a crucial communications pathway in cells not only stops cells from making proteins, it also makes them go.