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ATP and sugar monophosphates and the identification of a novel allosteric site on the vasopressin V2 receptor Discover how factors like restricted tissue diffusion and receptor density can dramatically alter drug The opioid crisis is evolving with the dangerous combination of fentanyl and the veterinary sedative Learn how fentanyl slows inhalation via opioid receptors, while xylazine prolongs exhalation through alpha-2 adrenergic receptors, creating a synergistic effect that drives overdose deaths.

High-throughput screening for receptor ligands was booming, and Sokhom was at the center of it. exploring signaling bias, and building a robust knowledge base in one of the most pharmacologically diverse receptor A Career Built on Consistency From CGRP receptor antagonists at BMS to opioid receptor research at Alkermes short-term thinkers often miss. _______________ Keyword Cloud: GPCR drug discovery , G protein-coupled receptors

What if you could directly measure receptor internalization in physiologically relevant cells without These probes become brighter and have a longer lifespan as internalized receptors enter acidic endosomes—translating his team presented a data set that transformed everything: a clean, dose-dependent response of GLP-1 receptor

shown in beta cells 🚀 2025: Revvity launches pHSense A Day That Changed Everything: The Endogenous Receptor s second “aha” moment with pHSense came the day his team showed internalization of endogenous GLP-1 receptors It validated the broader goal: giving scientists tools to study receptors in their native, unmodified

August 2022 "Emerging evidence suggests that G protein-coupled receptor (GPCR) kinases (GRKs) are associated

critical components of the intracellular signaling pathways that mediate the effects of G protein-coupled receptors For example, μ opioid receptor (MOR) interacts with Gαi/o and Gαz subunits, which have a slow enzymatic ; enhancing the activity of the G protein that is coupled to the receptor and leading to a decrease in Senese, N.B., et al., Regulator of G-Protein Signaling (RGS) Protein Modulation of Opioid Receptor Signaling Traynor, Differential modulation of mu- and delta-opioid receptor agonists by endogenous RGS4 protein

publications:  Studies on active-state GPCR ensembles and their transducer coupling, biased angiotensin receptor The Revvity team asked a harder question: What if you could measure receptor internalization in native The Advantages Live-cell imaging:  visualize receptor–ligand interactions in real time, without disturbing Subtype specificity:  selectively track receptor subtypes in complex brain tissue. Why It Matters In the CNS, where receptor localization and real-time signaling shape therapeutic outcomes

October 2022 "Protease-activated receptor 2 (PAR2) is a G-protein-coupled receptor (GPCR) activated by Interestingly, unlike PAR2-AP, GB83 and trypsin induced sustained receptor endocytosis and PAR2 colocalization

Consider G-protein-coupled receptors-an expansive class of transmembrane signaling proteins that participate While early evidence for the role of oligomerization in receptor signaling came from ensemble biochemical for these techniques to advance our understanding of the role of oligomerization in G-protein-coupled receptor

Considering the central role of the serotonin 5-HT2A receptor in the distinct effects of psychedelics

They’re kinetic game-changers —compounds that rewrite the relationship between ligand , receptor , and Understanding how persistent binding affects receptor turnover, tissue penetration, and PK/PD relationships This PK/PD dissociation  means: Drug exposure may end, but receptor occupancy remains. get released next month, featuring real questions from discovery scientists tackling enzyme kinetics, receptor Corner & Secure Your Spot for the October 30 AMA Why Terry’s Corner Pipeline risk isn’t just at the receptor—it

CRAC Motif in Transmembrane Helix 2 Confers Cholesterol-Induced Thermal Stability to the Serotonin 1A Receptor "G protein-coupled receptors (GPCRs) constitute the largest class of membrane proteins that transduce The serotonin1A receptor is a crucial neurotransmitter receptor in the GPCR family involved in a multitude In addition, we showed that membrane cholesterol stabilizes the serotonin1A receptor against thermal consensus (CRAC) motif in transmembrane helix 2 in conferring the thermal stability of the serotonin1A receptor

September 2022 "G-protein-coupled receptors (GPCRs) are involved in a wide array of physiological and Here, we find that protease-activated receptor 4 (PAR4) unexpectedly acts as a potent oncogene, inducing

October 2022 "Over three decades of research have provided thorough insights into G protein-coupled receptor Agonist activation of the β2-adrenoceptor (β2AR) causes its S-nitrosylation that is required for the receptor

Acquired hypocalciuric hypercalcemia (AHH) is a rare disease caused by calcium-sensing receptor (CaSR

Orthosteric ligands preempt  natural signaling; they “take over” receptor behavior, forcing physiology Allosterics , in contrast, act more like tuning knobs—modulating receptor ensembles in partnership with The Dynamic Nature of Receptor Binding Forget the static “lock-and-key” metaphor. Ligands bounce in and out of receptor sites, competing dynamically. By stabilizing certain receptor states over others, ligands literally remodel the energy landscape.

GPCR Store, and a spotlight on the cryo-EM structure of the sweet taste receptor.   Ben Clements   In Episode 166, Ben Clements dives into opioid pharmacology, GPCR-targeted PAMs, and how Show off your receptor pride and support the mission. The official Dr. GPCR Store is live! A stunning cryo-EM structure of the sweet taste receptor (TAS1R2–TAS1R3) shows how aspartame and sucralose Biased signalling of Class B G protein-coupled receptor-targeted therapeutics .  

studies of AlphaFold, RoseTTAFold and Modeller: a case study involving the use of G-protein-coupled receptors G-protein-coupled receptor (GPCR) proteins are particularly interesting since they are involved in numerous

intracellular allosteric binding site (IABS) has recently been identified at several G protein-coupled receptors Starting from vercirnon, an intracellular C-C chemokine receptor type 9 (CCR9) antagonist and previous

August 2022 "Background and purpose: Misuse of opioids has greatly affected our society. One potential solution is to develop analgesics that act at targets other than opioid receptors. These can be used either as stand-alone therapeutics or to improve the safety profile of opioid drugs Previous research showed that activation of Gq/11 proteins by G-protein coupled receptors has pro-nociceptive

G protein-coupled receptors (GPCRs) transmit extracellular signals to the inside by activation of intracellular Different agonists can promote differential receptor-induced signaling responses - termed bias - potentially Here, we compared the efficacy of seven agonists to induce G protein, G protein-coupled receptor kinase 2 (GRK2), as well as arrestin3 binding to the muscarinic acetylcholine receptor M3 by utilizing FRET-based to avoid differences in receptor phosphorylation influencing arrestin recruitment.

September 2022 "Melanocortin 4 receptor (MC4R) is part of the leptin-melanocortin pathway and plays an We have previously reported that the MC4R forms homodimers, affecting receptor Gs signaling properties protein–protein interaction were conducted, confirming decreased homodimerization capacities of chimeric receptors Gq/11 signaling of chimeric receptors was analyzed using luciferase-based reporter gene (NFAT) assays that inhibiting homodimerization has a setmelanotide-like effect on Gq/11 signaling, with chimeric receptors

August 2022 "The apelin receptor (APJ) is a target for cardiovascular indications.

Divergence, however, in the amino acid sequences of rodent and human PTH receptors (rat and mouse PTH1Rs are 91% identical to the human PTH1R) can lead to differences in receptor-binding and signaling potencies

the actions of hormones, neurotransmitters and other signaling molecules that bind G-protein coupled receptors

as a potential target in colorectal cancer using novel fluorescent GPCR ligands "G-protein coupled receptors We selected the adenosine receptor 2B (A2BAR), specifically expressed in cancer cell lines compared with Fluorescent probes allowed semi-quantitative receptor mapping in living cells and validated the specific As well, fluorescent ligands were effective at monitoring real-time A2BAR receptor labeling using live-imaging

their research on Functional consequences of spatial, temporal and ligand bias of G protein-coupled receptors Calebiro, Michael Decker, et al. for their study on Design, Synthesis, and Characterization of New δ Opioid Receptor-Selective Fluorescent Probes and Applications in Single-Molecule Microscopy of Wild-Type Receptors fibrosis progression Methods & Updates in GPCR Research Design, Synthesis, and Characterization of New δ Opioid Receptor-Selective Fluorescent Probes and Applications in Single-Molecule Microscopy of Wild-Type Receptors

October 2022 "Biased G protein-coupled receptor (GPCR) ligands, which preferentially activate G protein

October 2022 "The role of different G protein-coupled receptors (GPCRs) in the cardiovascular system In the former, stimulation of Gs-coupled receptors leads to increases in contractility, whereas stimulation of Gq-coupled receptors modulates cellular survival and hypertrophic responses. associated signaling machinery are localized in these cells with an emphasis on nuclear membrane-localized receptors

September 2022 "GPCRs are the most potential targets for drug discovery, however, their role in oncology is underappreciated and GPCR-based anti-cancer drug is not fully investigated. Herein, we identified GPR108, a GPCR protein described in innate immune system, is a potential therapeutic target of cancer. Depletion of GPR108 dramatically inhibited the survival of various cancers. Notably, TNFα activation of NF-κB was totally impaired after GPR108 knockout. We identified gambogic acid (GA), a natural prenylated xanthone, selectively targeting GPR108. Importantly, GA engaged with GPR108 and promoted its degradation, knockout of GPR108 remarkably blocked GA inhibition of NF-κB signaling. Furthermore, in vitro and in vivo assays demonstrated that GA was dependent on GPR108 to exert anti-cancer activity. Overall, our findings supported GPR108 as a promising therapeutic target of cancer, and provided a small molecule inhibitor GA directly and selectively targeting GPR108 for cancer therapy." Read more at the source #DrGPCR #GPCR #IndustryNews