Conformation- and activation-based BRET sensors differentially report on GPCR-G protein coupling Samuel Liu, Preston Anderson, Sudarshan Rajagopal, Robert Lefkowitz, Howard Rockman for their review G Protein-Coupled Receptors GPCR Event Highlight Join us for a special in-person event in collaboration with the Adhesion GPCR Consortium

September 2022 PLC-IP3-ORAI pathway participates in the activation of the MRGPRB2 receptor in mouse peritoneal

September 2022 "Background G protein-coupled receptor (GPCR) is the most targeted protein family by the FDA-approved drugs. GPCR-kinase 3 (GRK3) is critical for GPCR signaling. Our genomic analysis showed that GRK3 expression correlated with poor prognosis of gastric adenocarcinoma (GAC) patients. However, GRK3’s functions and clinical utility in GAC progression and metastases are unknown. Methods We studied GRK3 expression in normal, primary, and metastatic GAC tissues. We identified a novel GRK3 inhibitor, LD2, through a chemical-library screen. Through genetic and pharmacologic modulations of GRK3, a series of functional and molecular studies were performed in vitro and in vivo. Impact of GRK3 on YAP1 and its targets was determined." Read more at the source #DrGPCR #GPCR #IndustryNews

Preston Nibley, Dr. Sudha K Shenoy et al.

.; Rask-Andersen, M.; Schiöth, H. B.; Gloriam, D. E.

Liu S, Anderson PJ, Rajagopal S, Lefkowitz RJ, Rockman HA.