August 2022 "G-protein-coupled receptors (GPCR) are present at the cell surface in different conformational Here, we investigated this issue in living cells for the CC chemokine receptor 5 (CCR5), a major receptor in inflammation and the principal entry co-receptor for Human Immunodeficiency Viruses type 1 (HIV-1 We used TIRF microscopy and a statistical method to track and classify the motion of different receptor These results suggest a link between receptor activation and immobilization.

November 2022 "Despite the growing number of G protein-coupled receptor (GPCR) structures, only 39 structures

November 2022 "Dimerization of beta 2-adrenergic receptor (β2-AR) has been observed across various physiologies

September 2022 "The follicle-stimulating hormone receptor (FSHR) belongs to the glycoprotein hormone receptors, a subfamily of G-protein-coupled receptors (GPCRs). site and is linked to the transmembrane domain by the hinge region (HR), is characteristic for these receptors

cellular membrane's composition, organization, and physical properties might impact ligand binding, receptor membrane β-arrestin. β-arrestin reaches the receptor via lateral. Plasma membrane preassociation drives β-arrestin coupling to receptors and activation. Classical and new roles of b-arrestins in the regulation of G-protein-coupled receptors. Nat. Rev. Molecular mechanism of b-arrestin-biased agonism at seven-transmembrane receptors. Annu. Rev.

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.

October 2022 Cholesterol-Dependent Dynamics of the Serotonin1A Receptor Utilizing Single Particle Tracking : Analysis of Diffusion Modes "G protein-coupled receptors (GPCRs) are signaling hubs in cell membranes 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

"Pepducins are small-lipidated peptides designed from the intracellular loops of G protein-coupled receptors The effect of pepducins at their cognate receptors has been shown to vary between antagonist, partial This review will focus in particular on pepducins designed from protease-activated receptors, C-X-C motif chemokine receptors, formyl peptide receptors, and the β2-adrenergic receptor. We will discuss the historic context of pepducin development for each receptor, as well as the structural

October 2022 "Arrestins interact with G protein-coupled receptors (GPCRs) to stop G protein activation Here, we report the cryo-electron microscopy active structure of the wild-type arginine-vasopressin V2 receptor described GPCR-arrestin assemblies, associated with an original V2R/β-arrestin1 interface involving all receptor

October 2022 Glucagon receptor-mediated regulation of gluconeogenic gene transcription is endocytosis-dependent in primary hepatocytes "A number of G protein-coupled receptors (GPCRs) are now thought to use endocytosis We tested if this is true for the glucagon receptor (GCGR), which mediates physiological regulation of

Biosensors for monitoring G protein-coupled receptors (GPCRs), the most drugged class of proteins in briefly summarize a subset of this field with accelerating importance: transducer biosensors measuring receptor-coupling and selectivity, with an emphasis on sensors measuring receptor association and activation of heterotrimeric

August 2022 "As important drug targets, G protein-coupled receptors (GPCRs) play pivotal roles in a wide We revealed that AlphaFold2 could capture the overall backbone features of the receptors.

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.

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.

In this review, we focus on recent advances in G-protein-coupled receptor (GPCR) targets. To date, the most promising targets are the chemokine, cannabinoid, and dopamine receptors, but future work should further examine the melanocortin receptor-4 (MC4R), adhesion, lysophosphatidic acid (LPA ) and smoothened (Smo) receptors to initiate new drug-screening strategies and targeted delivery of safe

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

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

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

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

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.

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

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

He had engineered a mouse to make none of a particular receptor, a clean negative control, and yet several The receptors themselves often sit at very low abundance, so even finding a tissue that reliably presents And within a receptor family the sequences run so close, two chemokine receptors can share more than The receptor that taught GeneTex this most sharply was LGR5, a marker of adult stem cells that matters

tools—especially AlphaFold —are helping crack the mystery of olfactory GPCRs , one of the most elusive receptor The Problem: Hundreds of Receptors, Almost No Ligands Alessandro’s work focuses on olfactory GPCRs—nearly 400 distinct receptors that play key roles in smell but remain largely uncharacterized . Enter AlphaFold: Predicting the “Face” of a Receptor When Alessandro began his PhD, structural models From Prediction to Discovery One of Alessandro’s projects focused on receptor R5VK1 , where his team

Allostery isn’t just an advanced concept—it’s essential to understanding efficacy, ligand bias, and receptor Map dynamic receptor behavior to real-time decision-making.  

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