G protein-coupled receptors (GPCRs) are privileged structural scaffolds in biology that have
the versatility to regulate diverse physiological processes. Interestingly, many GPCR ligands …

Opioids are used for pain management despite the side effects that contribute to the opioid
crisis. The pursuit of non-addictive opioid analgesics remains unattained due to the …

Over one-third of current drugs target G-protein-coupled receptors (GPCRs). Leveraging the
phenomenon of biased signaling, where different ligands that bind to the same GPCR …

G protein–coupled receptors (GPCRs) are a superfamily of transmembrane signal
transducers that facilitate the flow of chemical signals across membranes. GPCRs are a …

Catecholamine-stimulated β2-adrenergic receptor (β2AR) signaling via the canonical Gs–
adenylyl cyclase–cAMP–PKA pathway regulates numerous physiological functions …

G protein-coupled receptors (GPCRs) are targeted by about a third of clinically used drugs.
Many GPCRs couple to more than one type of heterotrimeric G proteins, become …

Three classes of G-protein-coupled receptor (GPCR) partners–G proteins, GPCR kinases,
and arrestins–preferentially bind active GPCRs. Our analysis suggests that the structures of …

Arrestins are a small family of four proteins in most vertebrates that bind hundreds of
different G protein-coupled receptors (GPCRs). Arrestin binding to a GPCR has at least three …

The β-adrenergic receptors (βARs) include three subtypes, β 1, β 2 and β 3. These receptors
are widely expressed and regulate numerous physiological processes including …

Activation of β2-adrenoceptors (β2ARs) causes airway smooth muscle (ASM) relaxation and
bronchodilation, and β2AR agonists (β-agonists) are front-line treatments for asthma and …