September 2022 Isoforms of GPR35 have distinct extracellular N-termini that allosterically modify receptor-transducer coupling and mediate intracellular pathway bias "Within the intestine, the human G protein-coupled receptor activation and signaling of 10 different heterotrimeric G proteins, ligand-induced arrestin recruitment, and receptor results reveal that the extended N-terminus of the long isoform limits G protein activation yet elevates receptor-β-arrestin contributed by the extended N-terminus of the long GPR35 isoform limits the extent of agonist-induced receptor-β-arrestin2

, essential to maintaining proper cardiac output and circulation, is regulated by G protein-coupled receptor

Previously, we identified potent positive crosstalk between insulin/IGF-1 receptors and G protein-coupled

 Graham Ladds, and Antonios Kolocouris refine AlphaFold models using binding calculations for human adenosine A3 receptor. “ Dr. Classified GPCR News from January 22nd to 28th, 2024 GPCR Activation and Signaling Optical Control of Adenosine A2A Receptor Using Istradefylline Photosensitivity Comparative interactome analysis of α-arrestin families Structural and Molecular Insights into GPCR Function Optimizing cryo-EM structural analysis of Gi-coupling receptors

October 2022 "G protein-coupled receptors (GPCRs) are important drug targets characterized by a canonical impact of binding of agonists and antagonist/inverse agonists to selected structures of cannabinoid receptor 1 (CB1R), β2 adrenergic receptor (β2 AR) and A2A adenosine receptor (A2A AR). " Read more at the source

on the mechanism of signal activation, ligand selectivity and allosteric modulation in angiotensin receptors Thus, we need to know much more about the structures of receptor-ligand complexes at high resolution. Recently, X-ray structures of both AngII receptors (AT1 and AT2 receptors) bound to peptide and non-peptide , as the basis of ligand selectivity, efficacy, and regulation of the molecular functions of the receptors This review covers the new data elucidating the structural dynamics of AngII receptors and how structural

2022 N-terminal alterations turn the gut hormone GLP-2 into an antagonist with gradual loss of GLP-2 receptor selectivity towards more GLP-1 receptor interaction "Background and purpose: To fully elucidate the regulatory role of the GLP-2 system in the gut and the bones, potent and selective GLP-2 receptor (GLP To examine selectivity, COS-7 cells expressing human GLP-1 or GIP receptors were assessed for cAMP accumulation

pro-inflammatory neutrophil response, signaling downstream of an agonist-activated G protein-coupled receptor Among the family of GPCR kinases (GRKs) that regulate receptor phosphorylation and signaling termination The medium chain fatty acid receptor GPR84 as well as formyl peptide receptor 2 (FPR2), receptors expressed

Rho1 signaling is activated by G-protein-coupled receptor (GPCR) signaling at the cell surface. The SG receptor that transduces the Fog signal into Rho1-dependent myosin activation has not been identified

August 2022 "Emerging evidence suggests that G protein-coupled receptor (GPCR) kinases (GRKs) are associated

October 2022 "Protease-activated receptor 2 (PAR2) is a G-protein-coupled receptor (GPCR) activated by Interestingly, unlike PAR2-AP, GB83 and trypsin induced sustained receptor endocytosis and PAR2 colocalization

Consider G-protein-coupled receptors-an expansive class of transmembrane signaling proteins that participate While early evidence for the role of oligomerization in receptor signaling came from ensemble biochemical for these techniques to advance our understanding of the role of oligomerization in G-protein-coupled receptor

Considering the central role of the serotonin 5-HT2A receptor in the distinct effects of psychedelics

Nichola J Smith's investigation: Gene expression of TAS1R taste receptors for cardiometabolic disease psychosis risk factor RBM12 encodes a novel repressor of GPCR/cAMP signal transduction The relaxin receptor signals through a mechanism of autoinhibition To probe the activation mechanism of the Delta opioid receptor Development of an Affinity-Based Probe to Profile Endogenous Human Adenosine A3 Receptor Expression Pharmacokinetics and Pharmacodynamics of Burixafor Hydrobromide (GPC-100), a Novel C-X-C Chemokine Receptor

September 2022 Fentanyl activates ovarian cancer and alleviates chemotherapy-induced toxicity via opioid receptor-dependent

September 2022 "G-protein-coupled receptors (GPCRs) are involved in a wide array of physiological and Here, we find that protease-activated receptor 4 (PAR4) unexpectedly acts as a potent oncogene, inducing

CRAC Motif in Transmembrane Helix 2 Confers Cholesterol-Induced Thermal Stability to the Serotonin 1A Receptor "G protein-coupled receptors (GPCRs) constitute the largest class of membrane proteins that transduce The serotonin1A receptor is a crucial neurotransmitter receptor in the GPCR family involved in a multitude In addition, we showed that membrane cholesterol stabilizes the serotonin1A receptor against thermal consensus (CRAC) motif in transmembrane helix 2 in conferring the thermal stability of the serotonin1A receptor

October 2022 "Over three decades of research have provided thorough insights into G protein-coupled receptor Agonist activation of the β2-adrenoceptor (β2AR) causes its S-nitrosylation that is required for the receptor

Acquired hypocalciuric hypercalcemia (AHH) is a rare disease caused by calcium-sensing receptor (CaSR

intracellular allosteric binding site (IABS) has recently been identified at several G protein-coupled receptors Starting from vercirnon, an intracellular C-C chemokine receptor type 9 (CCR9) antagonist and previous

Jürgen Wess and Liu Liu for their study on A novel function of the M2 muscarinic receptor Drs. Zhan-Guo Gao, Mansour Haddad, and Kenneth A Jacobson for their work on A2B adenosine receptor signaling for breast cancer GPCR Activation and Signaling The TAS1R2 G-protein-coupled receptor is an ambient variants in the hypothalamic-pituitary-gonadal axis1 A novel function of the M2 muscarinic receptor A2B adenosine receptor signaling and regulation Novel medications for problematic alcohol use Structural

August 2022 "The apelin receptor (APJ) is a target for cardiovascular indications.

G protein-coupled receptors (GPCRs) transmit extracellular signals to the inside by activation of intracellular Different agonists can promote differential receptor-induced signaling responses - termed bias - potentially Here, we compared the efficacy of seven agonists to induce G protein, G protein-coupled receptor kinase 2 (GRK2), as well as arrestin3 binding to the muscarinic acetylcholine receptor M3 by utilizing FRET-based to avoid differences in receptor phosphorylation influencing arrestin recruitment.

studies of AlphaFold, RoseTTAFold and Modeller: a case study involving the use of G-protein-coupled receptors G-protein-coupled receptor (GPCR) proteins are particularly interesting since they are involved in numerous

cAMP assay: Temperature optimization and application to cell-based kinetic studies "G protein-coupled receptors (GPCRs) are an important receptor superfamily and common therapeutic targets. The second messenger cyclic adenosine monophosphate (cAMP) is a key mediator in many GPCR signaling pathways Temperature optimization studies were carried out using HEK293H cells transiently transfected with the adenosine receptor A2a and the GloSensor™ plasmid (pGloSensor-20F or -22F).

September 2022 "Melanocortin 4 receptor (MC4R) is part of the leptin-melanocortin pathway and plays an We have previously reported that the MC4R forms homodimers, affecting receptor Gs signaling properties protein–protein interaction were conducted, confirming decreased homodimerization capacities of chimeric receptors Gq/11 signaling of chimeric receptors was analyzed using luciferase-based reporter gene (NFAT) assays that inhibiting homodimerization has a setmelanotide-like effect on Gq/11 signaling, with chimeric receptors

Divergence, however, in the amino acid sequences of rodent and human PTH receptors (rat and mouse PTH1Rs are 91% identical to the human PTH1R) can lead to differences in receptor-binding and signaling potencies

the actions of hormones, neurotransmitters and other signaling molecules that bind G-protein coupled receptors