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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

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

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

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.

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).

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

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.  

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

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

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

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

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

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.

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

The sixth transmembrane region of a pheromone G-protein coupled receptor, Map3, is implicated in discrimination 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. Next, we swapped individual domains of Mam2 and Map3 with the respective domains in SoMam2 and SoMap3 , which revealed differences between the receptors both in the intracellular regions that regulate the

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

) that cause nephrogenic diabetes insipidus "Loss-of-function mutations of the arginine vasopressin receptor AVPR2 is a kind of G protein coupled receptor (GPCR) and mainly couples with Gαs protein leading to cAMP Investigation into the characterization of biased receptors may give insights into the relationship between the conformational change of the receptor because of the mutation and related downstream signaling. R68W showed bias to coupling with Gαq/11 protein rather than V162A and wild-type 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 (

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.

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).

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

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

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.

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

Numerous physiological effects of melatonin are mediated via its specific G protein-coupled receptors (GPCRs) named the MT1 receptor, which couples to both Gq and Gi proteins, and the MT2 receptor, which We investigated whether melatonin receptors are expressed on airway smooth muscle; whether they regulate We detected the mRNA and protein expression of the melatonin MT2 but not the MT1 receptor in native human Activation of melatonin MT2 receptors with either pharmacological concentrations of melatonin (10-100

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.

Obesity-induced changes in human islet G protein-coupled receptor expression: Implications for metabolic regulation G protein-coupled receptors (GPCRs) are a large family of cell surface receptors that are