G protein-coupled receptors (GPCRs) are the most intensively studied drug targets, mostly
due to their substantial involvement in human pathophysiology and their pharmacological …

A great deal of experimental evidence suggests that ligands can stabilize different receptor
active states that go on to interact with cellular signaling proteins to form a range of different …

Drugs targeting the μ-opioid receptor (μOR) are the most effective analgesics available but
are also associated with fatal respiratory depression through a pathway that remains …

Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …

Natural genetic variation in the human genome is a cause of individual differences in
responses to medications and is an underappreciated burden on public health. Although …

Endocannabinoids (eCBs) are retrograde neuromodulators with important functions in a
wide range of physiological processes, but their in vivo dynamics remain largely …

G-protein-coupled receptors (GPCRs) form the largest family of receptors encoded by the
human genome (around 800 genes). They transduce signals by coupling to a small number …

The control over the extent and timing of G protein signaling is provided by the regulator of G
protein signaling (RGS) proteins that deactivate G protein α subunits (Gα). Mammalian …

The recognition that individual GPCRs can activate multiple signaling pathways has raised
the possibility of developing drugs selectively targeting therapeutically relevant ones. This …

Recent studies have shown that G protein coupled receptors (GPCRs) show selective and
promiscuous coupling to different Gα protein subfamilies and yet the mechanisms of the …