September 2022 "G protein-coupled receptor (GPCR) kinases (GRKs) and arrestins mediate GPCR desensitization evidence that distal carboxyl-terminal tail (C-tail), but not proximal, phosphorylation of the chemokine receptor We demonstrate by pharmacologic inhibition of GRK2/3-mediated phosphorylation of the chemokine receptor CXCR4 coupled with site-directed mutagenesis and bioluminescence resonance energy transfer approaches that distal, not proximal, C-tail phosphorylation sites are required for recruitment of the adaptor protein

September 2022 "Given the promising clinical value of allosteric modulators of G protein-coupled-receptors (GPCRs), mechanistic understanding of how these modulators alter GPCR function is of significance. Here, we report the crystallographic and cryo-electron microscopy structures of the cannabinoid receptor the population of receptors that adopt an active conformation. Read more at the source #DrGPCR #GPCR #IndustryNews

meningitidis and identified 30 N-acyl amides with representative members serving as agonists of the G-protein coupled receptor (GPCR) S1PR4. Read more at the source #DrGPCR #GPCR #IndustryNews

"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 envision that our results could have potential implications in structural biological advancements of GPCRs and design of thermally stabilized receptors for drug development." Read more at the source #DrGPCR #GPCR #IndustryNews

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September 2022 GPCR/endocytosis/ERK signaling/S2R is involved in the regulation of the internalization We investigated the influence of specific inhibitors of G protein-coupled receptors (GPCR), endocytosis We performed a siRNA knockdown (KD) to assess the effect of Sigma-2 receptor (S2R) /Transmembrane Protein 97 (TMEM97)—a recently identified target protein of Hst1. Read more at the source #DrGPCR #GPCR #IndustryNews

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 Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Identification and functional characterization of the sulfakinin and sulfakinin receptor variety of behavioral processes and physiological functions in invertebrates through the interaction with G-protein-coupled receptors (GPCRs). Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Keratinocyte-derived defensins activate neutrophil-specific receptors Mrgpra2a/b to prevent Here, we discovered that the epithelial-cell-derived antimicrobial peptides defensins activated orphan G-protein-coupled receptors (GPCRs) Mrgpra2a/b on neutrophils. Read more at the source #DrGPCR #GPCR #IndustryNews

membrane and regulates epithelial apicobasal polarity "The adhesion family of G protein-coupled receptors These receptors are expressed widely and involved in various functions including development, angiogenesis stage of receptor biosynthesis. requires the C-terminal PDZ-domain-binding motif of GPR125 and its interaction with the cell polarity protein Thus, the basolateral protein GPR125, an autocleavable adhesion GPCR, appears to play a crucial role

September 2022 "The human sweet taste receptor is a heterodimeric receptor composed of two distinct G-protein-coupled receptors (GPCRs), TAS1R2 and TAS1R3. revealed that the VFT, CRR and TMD of TAS1R3 interact with some sweeteners, including the sweet-tasting protein Using size-exclusion chromatography coupled with light scattering, we found that hTAS1R2-VFT behaves Read more at the source #DrGPCR #GPCR #IndustryNews

GABAB receptors inhibit Ca2+ entry, whereas 5-HT1B receptors target SNARE complexes. We demonstrate in male and female rats that GABAB receptors receptors alter Pr, whereas 5-HT1B receptors Colocalization of different actions of GPCRs provide synaptic integration within presynaptic terminals Ca2+ In combination these pathways allow complex presynaptic integration.SIGNIFICANCE STATEMENTTwo G protein coupled receptors colocalize at presynaptic sites, to mediate presynaptic modulation by Gβγ,

June 2022 "G protein-coupled receptors (GPCRs) represent a major therapeutic target class as they play GPCRs are divided into six classes based on amino acid sequence similarities, but only four of the classes GPCRs respond to a wide variety of signals that range in size from photons to proteins (Foord et al., In 2019, 5 out of 20 first-in-class approved therapeutic agents targeted GPCRs. Read more at the source #DrGPCR #GPCR #IndustryNews

protein activity biosensors Descriptive molecular pharmacology of the δ opioid receptor (DOR): A computational Research High-throughput G protein-coupled receptor-based autocrine screening for secondary metabolite for the Treatment of Metabolic Disease Relevance of G protein-coupled receptor (GPCR) dynamics for receptor Protein-Coupled Receptor Influence of the Water Model on the Structure and Interactions of the GPR40 Announces Conference Call and Webcast of Second Quarter 2024 Financial Results G-Protein Coupled Receptors

ligand specificity and how binding affects the G-protein interface "Galanin is a neuropeptide expressed Three G-protein coupled receptors (GPCRs) for galanin have been discovered, which is the focus of efforts microscopy (cryo-EM) to solve the molecular structure of GALR2 bound to galanin and a cognate heterotrimeric G-protein inactive hβ2AR was used to relate galanin binding to the movements of transmembrane (TM) helices and the G-protein Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Fluorescently labeled ligands are versatile molecular tools to study G protein-coupled receptors (GPCRs) and can be used for a range of different applications, including bioluminescence resonance energy fluorescent ligands targeting the intracellular allosteric binding site (IABS) of the CC chemokine receptor 2 (CCR2), a class A GPCR that has been pursued as a drug target in oncology and inflammation. Read more at the source #DrGPCR #GPCR #IndustryNews

Protein Coupled Receptors (GPCRs): a historical perspective Monserrat Avila-Zozaya article on From DNA multiple G protein families Rapid elucidation of agonist-driven regulation of the neurokinin 1 receptor protein-coupled receptors in pain GPCRs in Oncology and Immunology Deciphering a GPCR-lncRNA-miRNA Nexus amplifying circuit enables sensitive detection of fungal pathogens In Silico Analyses of Vertebrate G-Protein-Coupled into Three Groups of Linkers Reviews, GPCRs, and more Deorphanization of G Protein Coupled Receptors

October 2022 "We describe production of the human A2A adenosine receptor (A2AAR), a class A G protein-coupled receptor (GPCR) for 19F-NMR and single-molecule fluorescence (SMF) spectroscopy. Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Computational study of the conformational ensemble of CX3C chemokine receptor 1 (CX3CR1 ) and its interactions with antagonist and agonist ligands "The CX3C chemokine receptor 1 (CX3CR1), a member of the class A of G Protein-Coupled Receptors (GPCR) superfamily, and its ligand fractalkine patterns that characterize a functional state to contribute to the understanding of the complexity of the GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "G protein-coupled receptors (GPCRs) are signaling hubs in cell membranes that regulate Serotonin1A receptors are important members of the GPCR family and are implicated in neuropsychiatric To explore the role of cholesterol in lateral dynamics of GPCRs, we utilized single particle tracking results bring out the interdependence of cholesterol and actin cytoskeleton in regulating diffusion of GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews

F-NMR and single-molecule fluorescence spectroscopy "We describe production of the human A2A adenosine receptor (A2AAR), a class A G protein-coupled receptor (GPCR) for 19F-NMR and single-molecule fluorescence (SMF Read more at the source #DrGPCR #GPCR #IndustryNews

GPCRs with receptor activity-modifying proteins Molecular mechanism of bitter taste receptor agonist-mediated Modulators GPCRs in Oncology and Immunology G protein-coupled receptor-mediated signaling of immunomodulation preferred human codon-optimized clytin II gene in Chinese hamster ovary-K1 cells and its use in the G-protein-coupled , GPCRs, and more G protein-coupled receptor (GPCR) gene variants and human genetic disease Advances in yeast synthetic biology for human G protein-coupled receptor biology and pharmacology Industry News

(LYCHOS, previously annotated as G protein-coupled receptor 155), a multidomain transmembrane protein that enables cholesterol-dependent activation of the master growth regulator, the protein kinase mechanistic concentrations, LYCHOS bound to the GATOR1 complex, a guanosine triphosphatase (GTPase)-activating protein Thus, LYCHOS functions in a lysosomal pathway for cholesterol sensing and couples cholesterol concentrations Read more at the source #DrGPCR #GPCR #IndustryNews

Specifically, we explore the role of actin cytoskeleton in regulating the dynamics of the serotonin1A receptor , a crucial neurotransmitter G protein-coupled receptor (GPCR) that plays a major role in the generation For this, we analyzed the lateral dynamics of the serotonin1A receptor in cholesterol-depleted cells in understanding the modulatory role of the membrane environment on the organization and dynamics of GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews

affect processes related to perception, cognition and sensory processing mostly via the serotonin 5-HT2A receptor Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "GPCRs are the most potential targets for drug discovery, however, their role in oncology is underappreciated and GPCR-based anti-cancer drug is not fully investigated. Herein, we identified GPR108, a GPCR protein described in innate immune system, is a potential therapeutic Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "Background G protein-coupled receptor (GPCR) is the most targeted protein family by the GPCR-kinase 3 (GRK3) is critical for GPCR signaling. Read more at the source #DrGPCR #GPCR #IndustryNews

includes their post-translational processing, release from dense core vesicles, and ability to activate G-protein-coupled receptors (GPCRs). Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE