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October 2022 "Visual phototransduction is the most extensively studied G protein-coupled receptor (GPCR

September 2022 Cannabinoid type-2 receptors: An emerging target for regulating schizophrenia-relevant brain circuits "Although the cannabinoid type-2 receptor (CB2) is highly expressed in the immune system Recent anatomical studies, combined with electrophysiological studies, indicate that CB2 receptors are effects of CB2 receptor activation, make this receptor an intriguing target for treating schizophrenia , has greatly advanced our understanding of this receptor.

September 2022 Expression pattern and clinical significance of beta 2-adrenergic receptor in oral squamous carcinoma: an emerging prognostic indicator and future therapeutic target "Purpose: Beta 2-Adrenergic Receptor

September 2022 β2-Adrenergic Receptor Expression and Intracellular Signaling in B Cells Are Highly Dynamic In the past, treatment of arthritic B cells with a β2-adrenergic receptor (β2-ADR) agonist has been shown Adrenergic receptors on B cells and intracellular β2-ADR downstream molecules (G protein-coupled receptor agonist terbutaline by flow cytometry. β2-ADR-expressing B cells increase during CIA without a change in receptor

September 2022 Sweet taste receptor agonists attenuate macrophage IL‐1β expression and eosinophilic inflammation were assessed using specific inhibitor, genetic knockdown or knockout, and overexpression of cognate receptors

This question led Huang et al., 2022 to investigate the molecular basis involved in G protein-receptor The binding pockets for serotonin were virtually identical between the receptor-Gs and receptor-Gi complexes The structural differences found between the receptor-Gs and receptor-Gi complexes evidenced that 5-HT4 is 7.5 residues shorter compared to 5-HT1/4 receptors that couple to Gi/o. Interestingly, in the case of promiscuous receptors they found that these receptors shared conserved

Integration and Spatial Organization of Signaling by G Protein-Coupled Receptor Homo- and Heterodimer complex organisms, cell to cell communication occurs mostly through neurotransmitters and hormones, and receptors The G protein-coupled receptors (GPCRs) are the largest family of membrane receptors, with nearly 800 evidence that supports these conjectures, fostering new ideas about the physiological role played by receptor

November 2022 "Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed this work, molecular docking screens for allosteric modulators targeting the metabotropic glutamate receptor The mGlu5 receptor is activated by the main excitatory neurotransmitter of the nervous central system , L-glutamate, and mGlu5 receptor activity can be allosterically modulated by negative or positive allosteric The mGlu5 receptor is a promising target for the treatment of psychiatric and neurodegenerative diseases

you interpret allosteric interactions —not as simple ligand displacement, but as transformations in receptor Become Something New In orthosteric pharmacology, a ligand is either on or off the receptor. But in allosteric systems , adding a modulator doesn’t push another molecule off—it transforms the receptor No matter how much non-radioactive ligand you add, the binding curve levels off —because the receptor Binding assays  report on one set of receptor states. Functional assays  track another.

August 2022 "Abstract The β3 -adrenergic receptor (β3 -AR) is found in several tissues such as adipose

identified 30 N-acyl amides with representative members serving as agonists of the G-protein coupled receptor

August 2022 "Fluorescently labeled ligands are versatile molecular tools to study G protein-coupled receptors fluorescent ligands targeting the intracellular allosteric binding site (IABS) of the CC chemokine receptor

August 2022 A correlation study of adhesion G protein-coupled receptors as potential therapeutic targets in Uterine Corpus Endometrial cancer "Adhesion G protein-coupled receptors (adhesion GPCRs), as a member of the G protein-coupled receptors (GPCRs) superfamily, have gradually entered the field of vision of

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

G protein-coupled receptor interactions and modification of signalling involving the ghrelin receptor , GHSR1a The growth hormone secretagogue receptor 1a (GHSR1a) is intriguing because of its potential Initial studies of the receptor focused on the potential therapeutic ability for growth hormone (GH) (GPCRs), including dopamine D1 and D2, serotonin 2C, orexin, oxytocin and melanocortin 3 receptors ( In all cases, the receptor interaction changes downstream signalling and the responses to receptor agonists

Involvement of various chemokine/chemokine receptor axes in trafficking and oriented locomotion of mesenchymal Chemokine and chemokine receptors are of the most important and effective molecules in MSC trafficking Chemokine/chemokine receptor axes play a pivotal role in the recruitment and oriented trafficking of immune cells both towards and within the CNS and it appears that chemokine/chemokine receptor signaling In this article, we hypothesized that the chemokine/chemokine receptor axes network have crucial and

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

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

G protein-coupled receptor signaling analysis using homogenous time-resolved Förster resonance energy This is moreso the case when detecting partial agonism or weak receptor interactions. , demonstrating high specificity and sensitivity in detecting ligand-receptor interactions.  A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery. A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery.

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.

systems, a ligand may appear to bind with very high affinity when it facilitates formation of ligand-receptor-G

Drug discovery often assumes receptor inhibition follows simple rules—agonist binds, antagonist blocks Ways Schild plots reveal hidden complexities like allosterism and receptor heterogeneity. No reduction  in the maximal response (the receptor can still be fully activated). Curvature  can signify heterogeneous receptors  or mixed response mechanisms. In practice, a deviation in slope or curvature isn’t noise—it’s the receptor speaking.

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

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