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 …

G protein coupled receptors (GPCRs) convey signals across membranes via interaction with
G proteins. Originally, an individual GPCR was thought to signal through one G protein …

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 …

Dopamine is a biologically active amine synthesized in the central and peripheral nervous
system. This biogenic monoamine acts by activating five types of dopamine receptors (D1 …

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

Abstract The Passerini–Smiles reactions of α‐ketophosphonates with nitrophenols has been
used as a platform to observe complex cascades involving multiple Smiles transfers coupled …

The discovery of functionally biased and physiologically beneficial ligands directed toward G-
protein coupled receptors (GPCRs) has provided the impetus to design dopamine D2 …

Compounds that target D2-like dopamine receptors (DRs) are currently used as therapeutics
for several neuropsychiatric disorders including schizophrenia (antagonists) and …

Highly selective dopamine D3 receptor (D3R) partial agonists/antagonists have been
developed for the treatment of psychostimulant use disorders (PSUD). However, none have …