October 2022 Regulation of pulmonary surfactant by the adhesion GPCR GPR116/ADGRF5 requires a tethered agonist-mediated activation mechanism "The mechanistic details of the tethered agonist mode of activation for the adhesion GPCR ADGRF5/GPR116 have not been completely deciphered. We set out to investigate the physiological importance of autocatalytic cleavage upstream of the agonistic peptide sequence, an event necessary for NTF displacement and subsequent receptor activation. To examine this hypothesis, we characterized tethered agonist-mediated activation of GPR116 in vitro and in vivo. A knock-in mouse expressing a non-cleavable GPR116 mutant phenocopies the pulmonary phenotype of GPR116 knock-out mice, demonstrating that tethered agonist-mediated receptor activation is indispensable for function in vivo. Using site-directed mutagenesis and species-swapping approaches, we identified key conserved amino acids for GPR116 activation in the tethered agonist sequence and in extracellular loops 2/3 (ECL2/3). We further highlight residues in transmembrane 7 (TM7) that mediate stronger signaling in mouse versus human GPR116 and recapitulate these findings in a model supporting tethered agonist:ECL2 interactions for GPR116 activation." Read more at the source #DrGPCR #GPCR #IndustryNews

the efficacy of seven agonists to induce G protein, G protein-coupled receptor kinase 2 (GRK2), as well

Data by Arne Hansen et a l has introduced a sensitive method for detecting GPCR mRNAs in human immune cells The study reports that human white blood cells express an average of 160 GPCR mRNAs, ranging from 123 , suggesting a potential role in regulating red blood cell production and offering a novel avenue for Additionally, the study identified unique expression patterns of GPCRs in different immune cell types , including B cells, CD4+ T cells, CD8+ T cells, natural killer (NK) cells, and dendritic cells.

of Technology in Genova, Italy (2008-2016) and an Associate Research Professor in the Department of Cell Biology at Duke University in North Carolina, USA (1996-2008). Before joining the Department of Cell Biology in 1996 as a postdoc and becoming faculty at Duke in 2000 As of August 2022, he has over 270 publications in scientific journals (including Science, Nature, Cell

Cardarelli is a drug development leader with extensive experience driving drug discovery teams in bringing biologics She has expertise in cell biology, pharmacology, translational medicine, oncology, immuno-oncology, immunology Previously, she held the position of Vice President of Cell Biology & Pharmacology, at Bristol-Myers She has extensive experience working with Biologics, and Antibody Drug Conjugates as well as experience

Beatriz Blanco Redondo The Adhesion GPCR Latrophilin Interacts With The Notch Pathway To Control Germ Cell Johannisallee 30, 04103 Leipzig, Germany 2Laboratory of Neurovascular Signaling, Department of Molecular Biology Biology, Department of Biology, Heinrich Heine University Düsseldorf, Düsseldorf, Germany 2 Rudolf Schönheimer Biology at Heinrich Heine University in Düsseldorf, Germany. Willem Berend Post on the web Cell Biology LinkedIn < Previous Session Next Session >