August 2022 "G-protein-coupled receptors (GPCRs) receive signals from ligands with different efficacies We report the cryo-EM structures of β1-adrenergic receptor (β1-AR) in complex with Gs (GαsGβ1Gγ2) and

cryogenic-electron microscopy (cryo-EM) is used extensively to determine structures of activated G protein-coupled receptors However, applying it to GPCRs without signaling proteins remains challenging because most receptors lack exploring different fusion protein designs, which lead to structures of antagonist bound A2A adenosine receptor

Prokineticins (PKs) exert their biological functions through the activation of the G protein-coupled receptors (GPCRs) prokineticin receptor 1 and 2 (PKR1, 2), and mutations in the PK2 and PKR2 genes are involved could assist the WAP domain both in the binding to PKR2 and in the modulation of the activation of the receptor

September 2022 Lack of Oestrogen Receptor Expression in Breast Cancer Cells Does Not Correlate with Kisspeptin Signalling and Migration "Kisspeptin is an anti-metastatic mediator in many cancer types, acting through its receptor been associated with increased invasion and MMP-9 expression, leading to the suggestion that hormone receptor veracity of this claim, we compared endogenous KISS1R signalling and physiological output in the hormone receptor-negative

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 In this work we present the study of the CX3CR1 receptor employing extensive atomistic Molecular Dynamics We analyzed the receptor conformational changes and described interactions within its key regions and

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 Our results show that the short-term diffusion coefficient of the receptor decreases upon cholesterol Analysis of SPT trajectories revealed that relative populations of receptors undergoing various modes Notably, in cholesterol-depleted cells, we observed an increase in the confined population of the receptor

The 5HT2C serotonin receptor, which undergoes 32 distinct RNA-editing events leading to 24 protein isoforms

September 2022 PLC-IP3-ORAI pathway participates in the activation of the MRGPRB2 receptor in mouse peritoneal mast cells "A novel mast cell-specific G-protein-coupled receptor (GPCR), known as Mas-related G protein-coupled receptor-B2 (MRGPRB2), plays important roles in immune response.

September 2022 "The human sweet taste receptor is a heterodimeric receptor composed of two distinct G-protein-coupled receptors (GPCRs), TAS1R2 and TAS1R3. acid substitutions (D278A and E382A) known to abolish the response of the full-length TAS1R2/TAS1R3 receptor

Bursicon receptor gene HLGR2 as a potential RNA interference target for control of the fall webworm Hyphantria cunea Background: Insect G protein-coupled receptors (GPCRs) have been identified as a new generation

Mutations in G protein-coupled receptors (GPCRs) underlie numerous diseases. Many cause receptor misfolding and failure to reach the cell surface. We previously demonstrated rescue of cell surface expression of luteinizing hormone receptor mutants we demonstrate that a similar approach can be employed to rescue mutant follicle-stimulating hormone receptors

affect processes related to perception, cognition and sensory processing mostly via the serotonin 5-HT2A receptor

August 2022 Dopamine D 1 receptor-mediated β-arrestin signaling: Insight from pharmacology, biology, A major pan-receptor focus has been to identify GPCR-selective ligands that have bias in G protein-dependent the past two decades, it is only recently that highly β-arrestin biased ligands for the dopamine D1 receptor

October 2022 Keratinocyte-derived defensins activate neutrophil-specific receptors Mrgpra2a/b to prevent that the epithelial-cell-derived antimicrobial peptides defensins activated orphan G-protein-coupled receptors

October 2022 Focusing on the role of secretin/adhesion (Class B) G protein-coupled receptors in placental G protein-coupled receptors, the largest family of membrane proteins in eukaryotes and the largest drug Among them, the secretin/adhesion (Class B) G protein-coupled receptors are essential drug targets for Given the great value of the secretin/adhesion (Class B) G protein-coupled receptors in the regulation of cardiovascular system function and the drug target exploration, we summarize the role of these receptors

Bitter taste receptors (TAS2Rs) are a poorly understood subgroup of G protein-coupled receptors (GPCRs The experimental structure of these receptors has yet to be determined, and key-residues controlling

September 2022 Cell Surface Calcium-Sensing Receptor Heterodimers: Mutant Gene Dosage Affects Ca 2+ Sensing but Not G Protein Interaction "The calcium-sensing receptor is a homodimeric class C G protein-coupled receptor (GPCR) that senses extracellular Ca2+ (Ca2+o ) via a dimeric extracellular Venus flytrap (VFT severe hyperparathyroidism (NSHPT), receptor function was markedly impaired. We consider how receptor asymmetry may support the underlying mechanisms. © 2022 The Authors.

September 2022 Structure of the human galanin receptor 2 bound to galanin and Gq reveals the basis of Three G-protein coupled receptors (GPCRs) for galanin have been discovered, which is the focus of efforts To understand the basis of the ligand preferences of the receptors and to assist structure-based drug

September 2022 "The GPR15 receptor is a G protein-coupled receptor (GPCR), which is activated by an endogenous However, the activation profiles of the GPR15 receptor within Gi/o subtypes have not been examined. Moreover, whether the receptor can also couple to Gs , Gq/11 and G12/13 is unclear. The results show that the GPR15 receptor preferentially couples to Gi/o rather than other pathways in Within the Gi/o family, the GPR15 receptor activates all the subtypes (Gi1 , Gi2 , Gi3 , GoA , GoB and

September 2022 "The glucagon-like peptide-1 receptor (GLP-1R) plays a key role in metabolism and is an

HEK293 cells reveals that both conventional and novel protein kinase C isozymes are involved in mGlu5a receptor internalization "The internalization of G protein-coupled receptors (GPCRs) can be regulated by PKC. to investigate the contribution of PKC isozymes in the internalization of the metabotropic glutamate receptor Direct activation of PKC and mutation of rat mGlu5a Ser901, a PKC-dependent phosphorylation site in the receptor C-tail, both showed that PKC isozymes facilitate approximately 40% of the receptor internalization.

August 2022 "Abstract Sigma receptor is a transmembrane non-GPCR protein expressed mainly in the endoplasmic

Alterations in the expression and/or activity of brain G-protein-coupled receptors (GPCRs) such as dopamine functional role of kurarinone, an abundant lavandulated flavonoid in Sophora flavescens, on dopamine receptor

In this sense, G protein-coupled receptors (GPCRs) may be a good option to try to prolong our life while

Self-docking and cross-docking simulations of G protein-coupled receptor-ligand complexes: Impact of ligand type and receptor activation state G protein-coupled receptors (GPCR) are the largest family of cell surface receptors in vertebrates. Likewise, the relative importance of receptor activation state and ligand function differences have also Receptor conformational sampling in advance of docking or receptor conformational adjustment after docking

Crystal structures suggest ligand access to the orthosteric binding site of MT1 and MT2 receptors through entry route for 2-iodomelatonin, a nonselective agonist with a slower dissociation rate from the MT2 receptor which revealed different trajectories passing through the gap between TM helices IV and V for both receptors The side-chain flexibility of Tyr5.38 was significantly different in the two receptor subtypes, as assessed is a way of connecting the orthosteric binding site and the membrane core for lipophilic melatonin receptor

sympatholytic treatments (such as β-blockers) and renin-angiotensin system inhibitors or mineralocorticoid receptor Synthesis and release of these hormones in the adrenals is tightly regulated by adrenal G protein-coupled receptors (GPCRs), such as adrenergic receptors and AngII receptors. context of chronic HF, by focusing on the 2 best studied adrenal GPCR types in that context, adrenergic receptors and AngII receptors (AT 1 Rs).

neurotrophic factor-α1 (NF-α1/carboxypeptidase E, CPE) and human 5-HTR1E, a G protein-coupled serotonin receptor Thus, NF-α1/CPE uniquely interacts with serotonin receptor 5-HTR1E to activate the β-arrestin/ERK/CREB