Overview of G-Protein Coupled Receptor

GPCR Inhibition in Treating Lymphoma

“…Besides G-protein, GPCRs can also mediate signal through β-arrestins, multifunctional adaptor proteins that activate several signaling molecules such as c-Src, extracellular regulated kinase (ERK), Janus-activated kinase (JNK), and small GTPase RhoA by forming a complex with them. Some GPCR ligands activate either G-protein or β-arrestin; this event is called as “biased activation” …”

“…Some GPCR ligands activate either Gprotein or β-arrestin; this event is called as "biased activation". 2 Due to the key roles of GPCRs in cell physiology and homeostasis, altered signaling pathways associated with GPCRs are implicated in the pathophysiology of various diseases, including cancer, infections, and metabolic, immunological, or neurodegenerative disorders. Approximately 40% of clinically approved drugs mediate their effects by modulating GPCRs, which makes them attractive targets for drug screening and discovery.…”

“…Some GPCR ligands activate either G-protein or β-arrestin; this event is called as “biased activation”. 2 …”