Molecular Modeling Study of a Receptor-Orthosteric Ligand-Allosteric Modulator Signaling Complex. Updates in GPCR Research Development and Characterization of a Highly Selective Turn-On Fluorescent Ligand GPCR Signaling Measurement and Drug Profiling with an Automated Live-Cell Microscopy System. (May 22 - 26, 2023) 2nd LEAPS Meets Life Sciences Conference. regulation of GPCR signalling Postdoctoral Fellow - Molecular Dynamics Postdoc in lipid regulation of

Revealing the tissue-level complexity of endogenous glucagon-like peptide-1 receptor expression and signaling structural arrangement of cells and collective calcium transients: an integrated framework combining live Targeting in silico GPCR conformations with ultra-large library screening for hit discovery. Ligands selectively tune the local and global motions of neurotensin receptor 1 (NTS1). (May 22 - 26, 2023) 2nd LEAPS Meets Life Sciences Conference.

Hello Readers👋, We are working on bringing your the latest GPCR News more frequently directly in your the Formation of a Cross-Functional Scientific and Drug Discovery Advisory Board Sosei Heptares and Lilly Enter Multi-target Collaboration and License Agreement in Diabetes and Metabolic Diseases Sosei Heptares

Activity-Modifying Phosphorylation Barcode in a Class C G Protein-Coupled Receptor Reviews, GPCRs, and more Life resurrection of plant GPCRs Structural and Molecular Insights into GPCR Function Synergistic and Competitive Lipid

November 2022 "Some G protein-coupled receptor (GPCR) ligands act as "biased agonists" that preferentially differential subcellular signaling contributes to the biased signaling generated by three endogenous ligands The signaling profile of CXCR3 changes as it traffics from the plasma membrane to endosomes in a ligand-specific

HH controls SMO subcellular localization and activity in a polarized epithelium using the Drosophila wing Together, these results link the morphogenetic effects of HH to the apico-basal distribution of SMO and

Recent structural studies shed light on the molecular mechanisms involved in GPCR-arrestin coupling,

cryo-ET) data on the ROS with structural knowledge on individual proteins to define the precise spatial limitations

It is activated by the three chemokine ligands CXCL9, CXCL10, and CXCL11 and enables the recruitment

Recurrent hypoglycemia increases hepatic gluconeogenesis without affecting glycogen metabolism or systemic lipolysis : To study the effects of RH on metabolic pathways associated with glucose counterregulation within liver their inhibitory regulators and downstream enzymes catalyzing glycogen metabolism, gluconeogenesis and lipolysis Additionally, we measured circulating FFA and glycerol to check lipolysis.

However, the available tools to dissect the endogenous dopaminergic circuits have limited specificity Here, we introduce azodopa, a novel photoswitchable ligand that enables reversible spatiotemporal control We demonstrate that azodopa activates D1-like receptors in vitro in a light-dependent manner.

from camelids, have become indispensable tools for interrogating GPCRs both in purified systems and in living

In this review, we provide an accessible summary of the literature on Alzheimer's disease and the therapeutic

and promotes expression of phosphoenolpyruvate carboxykinase 1 (PCK1), the enzyme catalyzing the rate-limiting

We generated mutant mouse lines lacking the entire Defensin (Def) gene cluster in keratinocytes or Mrgpra2a

In rodents, intrathecal injection of its ligand, 7α,25-dihydroxycholesterol (7α,25-OHC), causes time-dependent

However, most tools available to study the contribution of PKC isozymes have considerable limitations In this study, we generated and characterized human embryonic kidney 293A (HEK293A) cell lines devoid Our PKC KO cell lines expand the repertoire of KO HEK293A cell lines available to research GPCR pharmacology pharmacological tools to study PKC isozymes generally lack specificity and/or potency, we present the PKC KO cell lines

structures of B2R have provided molecular insights into the functions and regulation of B2R, which shed light

interaction of VLGR1 with key proteins of MAMs by pull-down assays in vitro complemented by in situ proximity ligation Immunocytochemistry by light and electron microscopy demonstrated the localization of VLGR1 in MAMs.

assays were performed using PBMCs isolated from these individuals in response to the synthetic GPR15 ligand

surgery is the cooperative improved action of the preproglucagon-derived hormones, glucagon, glucagon-like

the first receptors shown to transactivate other receptors: noticeably, these interactions are not limited

We also showed that the EMC promotes surface expression of C3aR, likely explaining its identification

presence of CaSR autoantibodies that operated as biased allosteric modulators of CaSR, and (g) were likely

A diverse pharmacopoeia of cannabinoid ligands is available, which has led to considerable advancements However, until recently, most CB2 ligands were highly lipophilic and as such not optimal for clinical A number of strategies have been applied to develop CB2 ligands to achieve closer to 'drug-like' properties We review the current state of CB2 ligand development and progress in optimising physicochemical properties

October 2022 "Pepducins are small-lipidated peptides designed from the intracellular loops of G protein-coupled

unveiled a new antifibrotic cGAS/STING signaling pathway that suppresses pathological angiogenesis in liver We showed that cGAS expression was induced in fibrotic liver and kidney, but suppressed in endothelial cells. cGAS genetic deletion promoted liver and kidney fibrosis and pathological angiogenesis, including receptor (GPCR)-based antagonist that blocks the profibrotic activity of endothelial YAP, attenuated liver Further, pharmacological targeting of cGAS/STING-YAP axis exhibits the potential to alleviate liver and

October 2022 "Biased G protein-coupled receptor (GPCR) ligands, which preferentially activate G protein However, Gpr3-deficient mice display several adverse phenotypes, including elevated anxiety-like behavior by robust microglial and astrocytic hypertrophy, which suggest a protective glial response that may limit