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 …

Constitutive receptor activity/inverse agonism and functional selectivity/biased agonism are
2 concepts in contemporary pharmacology that have major implications for the use of drugs …

G protein-coupled receptors (GPCRs) signal through both G-protein-dependent and G-
protein-independent pathways, and β-arrestin recruitment is the most recognized one of the …

Traditionally, drugs are monovalent, targeting only one site on the protein surface. This
includes orthosteric and allosteric drugs, which bind the protein at orthosteric and allosteric …

G protein-coupled receptors (GPCRs), the largest family of human membrane proteins and
an important class of drug targets, play a role in maintaining numerous physiological …

The genesis of designing bivalent or bitopic molecules that engender unique
pharmacological properties began with Portoghese's work directed toward opioid receptors …

Adenosine modulates many aspects of human physiology and pathophysiology through
binding to the adenosine family of G protein-coupled receptors, which are comprised of four …

Biased signalling is a natural result of GPCR allosteric function and should be expected from
any and all synthetic and natural agonists. Therefore, it may be encountered in all agonist …

Highlights•GPCRs, a superfamily of membrane proteins, are vital for multiple signaling
pathways related to human physiology.•GPCR activation induces conformational changes …

The development of therapeutic agonists for G protein-coupled receptors (GPCRs) is
hampered by the propensity of GPCRs to couple to multiple intracellular signalling …