Identification of a heparan sulfate proteoglycan with a dedicated function in unconventional protein secretion reveals an intimate relationship between fibroblast growth factor 2 and Glypican-1 in cancer biology.
Lindsay D Clark, Igor Dikiy ... Daniel M Rosenbaum
Generation of a highly deuterated 13C-methyl labeled wild-type GPCR sample is used to facilitate characterization of the molecular environments and fast ps-ns dynamics of sidechains when the receptor is bound to ligands of different efficacy.
Trisha V Vaidyanathan, Max Collard ... Kira E Poskanzer
Cortical astrocytes play key roles in NREM sleep by regulating sleep depth and duration through separate GPCR pathways, and differentially control neuronal slow-wave activity in local and remote cortical circuits.
A polarized Moody/protein kinase A pathway plays an unrecognized central role in controlling the enormous cell growth and blood–brain barrier integrity in a highly coordinated spatiotemporal manner in brain homeostasis.
Alexander S Hauser, Charlotte Avet ... David E Gloriam
The GPCR-G protein coupling map and selectivity insights will catalyze advances in receptor research, cellular signaling, and drug discovery exploiting G protein signaling bias to design safer drugs.
The safety and strong antitumor effects of GPC1-specific CAR-T cells against GPC1-expressing solid tumors were demonstrated by using both syngeneic and xenogeneic mouse models.
Heparan Sulfate Proteoglycans function as receptors for the R-spondins, a family of growth factors that amplify the strength of WNT signaling during development and in adult stem cells.
An interdisciplinary approach uncovers a new antinociceptive molecular mechanism and shows that the adhesion GPCR CIRL adjusts the sensation of gentle touch and noxious mechanical insult in opposite directions.
James P Bridges, Caterina Safina ... Marie-Gabrielle Ludwig
Mutagenesis and activity assays in vitro and in vivo identify residues in the tethered agonist of GPR116, as well as those within the extracellular loops, that are critical for mediating the response to the tethered agonist.