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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

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

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

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

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

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

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

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.

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

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

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.  

The company’s scientific approach relied on targeting GPCRs — specifically opioid receptors — using biased The company’s goal is to model receptor dynamics — including biased signaling — to predict drug behavior Superluminal is building systems that learn from receptor movement, conformational shifts, and complex By making receptor behavior computationally predictable, Ajay and his team are working to reduce the

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).

Bigger Picture: GPCR Science Meets Public Health At its core, Catherine Demery’s research  is about receptors and signaling pathways—how mu-opioid  and alpha-2 adrenergic receptors  interact to disrupt breathing Fentanyl, through the mu-opioid receptor, blunts the brainstem’s inspiratory drive so that each breath By displacing opioids from the mu-opioid receptor, it restores breathing within minutes. But that mechanism has no impact on xylazine, which works through alpha-2 adrenergic receptors.

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

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

Intracellular Molecular Glues Classic models explain biased signaling through ligands that stabilize receptor NTSR1 and PCO371 at PTH1R , already characterized, provide concrete cases where ligands engage both receptor Key implications: SBI-553 illustrates how arrestin signaling can be stabilized through direct receptor–Gαo This limitation affects how signaling data can be interpreted when receptor behavior depends on cell ligands, while functional assays measure the receptor population that couples to signaling pathways.

August 2022 "Opioid receptors (ORs) represent one of the most significant groups of G-protein coupled receptor (GPCR) drug targets and also act as prototypical models for GPCR function.

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

Questions about how opioids impair breathing, why xylazine complicates interventions, and how receptor-level This approach makes her models not just rigorous, but translational—bridging the gap between receptor She is especially interested in mu-opioid receptor signaling  and how xylazine, as an alpha-2 adrenergic That personal loss transforms complex receptor pharmacology into something immediate and human.

Breakthroughs this week: Structure-based discovery of positive allosteric modulators of the A1 adenosine receptor Identify emerging targets:  Allosteric modulators, biased ligands, and kinetic frameworks will dominate

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).

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

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

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

exactly as the underlying system allowed—amplified, buffered, redirected, or reshaped by layers of receptor How enzyme behavior introduces nonlinear risk even in receptor-driven programs. Physiological reflexes instantly counteract, amplify, or redirect receptor-level effects. Multi-receptor involvement—intentional or not—often dictates the phenotype. Interrogate agonists across multiple receptor-expression states.

When pharmacologists misinterpret how an antagonist interacts with its receptor, the consequences ripple But if the antagonist binds tightly and dissociates slowly, the receptor remains blocked, even at high Antagonist “hogs” the receptor, depressing the response, even if more agonist is added. Common misconceptions  arise when irreversible binding, receptor reserve, or allosteric effects mimic He challenges the idea that curve shape alone is diagnostic, pointing out how features like receptor

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

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