… GPCR allosteric ligands, which is critical for discovering novel therapeutics. This book chapter
summarized different GPCR allosteric … on allosteric modulator-GPCR complex structures. …

… of the basics of GPCR allosteric pharmacology, medicinal chemistry, … recent advances in the
discovery of allosteric ligands for … new advances with allosteric ligands for other GPCRs and …

… biased allosteric modulation, highlight … allosteric GPCR ligands. As their potential value in
creating safer therapies is realized, BAMs may well sustain a new era of GPCR drug discovery. …

… , the discovery and understanding of allosteric modulators have gained tremendous momentum,
and GPCR allosteric modulators are … To date, no GPCR allosteric modulators have been …

… allosteric sites in GPCRs, including “orphan” allosteric pockets … map the entire GPCR
pocketome based on available GPCR … approaches for the discovery of allosteric modulators for the …

… , intense discovery efforts for several GPCR subtypes have … Historically, drug discovery
programmes for GPCR ligands … the discovery of novel ligands for GPCRs that act at allosteric sites …

… and is proving to be a viable drug discovery strategy, as evidenced by … GPCR allosteric
modulators have been discovered recently, and emerging trends such as the availability of GPCR …

… It is conceivable that dimer stabilization (via ligand chaperone activity) or dimer prevention
with rationally designed allosteric modulators could be an attractive drug discovery strategy in …

… Both binding and functional assays have specific advantages when they are used to
screen for allosteric modulators of GPCRs. However, the extent and direction (that is, positive, …

… to the field of drug discovery. In this section, the GPCRs allosteric modulation will be
specified in the following three aspects: GPCRs structural biology with the focus on locations of …