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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

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

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

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

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.

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

Breakthroughs this week: Structure-based discovery of positive allosteric modulators of the A1 adenosine receptor

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

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

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

why two drugs with similar affinity may behave completely differently , and how the secret lies in receptor In this session, you’ll gain: ✅ A deeper understanding of how every ligand alters receptor conformation—and Ligands don’t just “bind”—they change  the receptor. These changes can alter how the receptor talks to G proteins, arrestins, or other receptors. receptors, where ligand context fundamentally changes modulator behavior.

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

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

September 2022 Cell-Type-Specific Effects of the Ovarian Cancer G-Protein Coupled Receptor (OGR1) on Proton-sensing G-protein coupled receptors are activated by acidic environments, but their role in fibrosis Here, we report that the Ovarian Cancer G-Protein Coupled Receptor1 (OGR1 or GPR68) has dual roles in

September 2022 A2B Adenosine Receptor Enhances Chemoresistance of Glioblastoma Stem-Like Cells under we show for the first time that MRP3 expression is induced under hypoxia through the A2B adenosine receptor Downregulation of the A2B receptor decreases MRP3 expression and chemosensibilizes GSCs treated with These data suggest that hypoxia-dependent activation of A2B adenosine receptor promotes survival of GSCs

Mitogen-Activated Protein Kinase and Nuclear Factor- κ B "Emerging evidence implicates the G-protein coupled receptor

August 2022 "The atypical chemokine receptor 1 (ACKR1) was discovered on erythrocytes as the Duffy blood group antigen ( Cutbush et al., 1950 ), also called Duffy-antigen/receptor for chemokines, or DARC (

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 GABAB receptors alter Pr leaving synaptic properties unchanged, while 5-HT1B receptors fundamentally change properties of synaptic transmission, modifying AMPA receptor but sparing NMDA receptor responses Co-activation of these receptors allows synaptic integration because of convergence of GABAB receptor

by sea bass gonadotropin-inhibitory hormone peptides in COS-7 cells transfected with their cognate receptor significantly decreased forskolin-elicited CRE-luc activity in COS-7 cells transfected with their cognate receptor Notably, GnIH2 antagonized Kiss2-evoked CRE-luc activity in COS-7 cells expressing GnIHR and Kiss2 receptor

The sixth transmembrane region of a pheromone G-protein coupled receptor, Map3, is implicated in discrimination the molecular recognition of two peptidyl mating pheromones by their corresponding G-protein coupled receptors Although such pheromone/receptor systems are likely to function in both mate choice and prezygotic isolation , very few studies have focused on the stringency of pheromone receptors. GPCRs might reflect the significantly distinct stringency/flexibility of their respective pheromone/receptor

The company has long-standing expertise in G protein–coupled receptor (GPCR) biology—one of the most capabilities span the full spectrum of GPCR families, including aminergic, peptide, lipid, and chemosensory receptors (such as bitter and metabolic receptors).

conditions, what appears to be a second high-affinity site may simply reflect kinetic factors—such as ligand-receptor-G

Nanobody binding stabilizes G-protein-coupled receptors (GPCR) in a fully active state and modulates conformational changes induced by the binding of a nanobody (Nb80) on the active-like β2 adrenergic receptor proximity of transmembrane (TM) helices 5 and 7, and favors the fully active-like conformation of the receptor contrast to the conditions under which no intracellular binding partner is bound, in which case the receptor intracellular loop 2 and extracellular loop 2 are captured from the trajectories of various ligand-bound receptors