… G protein-coupled receptors (GPCRs), the largest … of allosteric regulation. More importantly,
this review highlights the diversity of allosteric sites and presents how allosteric modulators …

… growth in the identification of allosteric modulators of G protein–coupled receptors (GPCRs), …
by the receptor's endogenous agonist. Because of their ability to modulate receptor …

… G protein-coupled receptors (GPCRs),4 also known as 7-transmembrane (7TM) … signaling
pathways, indicating that allosteric modulation of discrete allosteric sites may have significant …

… allosteric modulator B interact with their respective binding sites on the unoccupied receptor,
R… the quantification of allosteric effects at some GPCRs, allosteric modulators are now being …

… G protein-coupled receptor (GPCR)-based drug discovery has traditionally focused on
targeting the orthosteric site for the endogenous agonist. However, many GPCRs …

… allosteric effects, based on an increased awareness of various mechanisms underlying
allosteric modulator … the current paucity of GPCR allosteric modulators in the clinical setting and …

… be noted that G protein coupling and signal transduction for receptors in the … allosteric
modulators have been described for receptors in the Rhodopsin, Secretin and Glutamate receptor …

… Schematic diagram of the model for allosteric binding to an allosteric modulator (B) to a
receptor (R) and an endogenous agonist (A). The affinity of the receptor for each ligand is …

… Allosteric modulation of G protein-coupled receptors has … In this overview, allosteric modulators
that enhance or … on a variety of G protein-coupled receptors are described. Emphasis is …

… Although a further and more detailed examination of receptor theory and allosteric modulator
activity modeling is clearly beyond the scope of this Review, readers are referred to a …