Dysregulation of peptide-activated pathways causes a range of diseases, fostering the
discovery and clinical development of peptide drugs. Many endogenous peptides activate G …

As important drug targets, G protein-coupled receptors (GPCRs) play pivotal roles in a wide
range of physiological processes. Extensive efforts of structural biology have been made on …

G protein-coupled receptors (GPCRs) are physiologically abundant signaling hubs routing
hundreds of extracellular signal substances and drugs into intracellular pathways. The …

G protein-coupled receptors (GPCRs) form both the largest family of membrane proteins and
drug targets, mediating the action of one-third of medicines. The GPCR database, GPCRdb …

Two-thirds of human hormones and one-third of clinical drugs activate~ 350 G-protein-
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …

Despite intense interest in expanding chemical space, libraries containing hundreds-of-
millions to billions of diverse molecules have remained inaccessible. Here we investigate …

Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …

Abstract Serotonin, or 5-hydroxytryptamine (5-HT), is an important neurotransmitter, that
activates the largest subtype family of G-protein-coupled receptors. Drugs that target 5 …

Because nonopioid analgesics are much sought after, we computationally docked more
than 301 million virtual molecules against a validated pain target, the α2A-adrenergic …

Adhesion G-protein-coupled receptors (aGPCRs) are important for organogenesis,
neurodevelopment, reproduction and other processes,,,,–. Many aGPCRs are activated by a …