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G protein-coupled receptors (GPCRs) are integral to cellular signaling, influencing a wide array of physiological The researchers found that certain GPCRs, such as vasopressin receptors, were expressed in hematopoietic For instance, the expression of specific chemokine receptors in monocytes and macrophages indicates their The current study found that 133 of these receptors were also detected, highlighting the robustness of However, the study also noted discrepancies, with 26 receptors identified in the previous study not detected

Adenine-derived scaffolds enabled selective adenosine receptor antagonists; tryptophan modifications led to somatostatin receptor ligands.  The molecule, not the receptor, becomes the guiding principle. Does it interact with the receptor in a way that biology can use? Core message: The receptor is only half the story. The molecule is the other half.

Administration (FDA) for use in adults for the management of acute pain severe enough to require an intravenous opioid

In the case of fluorescent ligands , where a fluorescent tag is attached to a pharmacophore , the receptor This provides flexibility in labelling the GPCRs but may interfere with functional activity of the receptors If the experiment is done on live cells , tracking real-time receptor internalization becomes possible On the other hand, in fixed cells studies, it facilitates the structural context necessary to map receptor A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery.

Hodson’s work with a major scientific wave: The rise of incretin-based therapies, especially GLP-1 receptor Receptor localization, ligand access, and intracellular signaling can look different in actual tissues For real translational understanding, you need to see  the receptor in context. Emerging direction: Genetics + receptor-distribution mapping. The next breakthroughs will come not from new receptors , but new ways of engaging and combining the

For a field that depends on understanding where receptors actually are — and how many are available at They could be engineered to target surface-exposed receptors, remain stable across batches, support live-cell Receptors internalize, traffic, recycle, and degrade. The work now stretches far beyond a single receptor. They’re also performing increasingly complex imaging experiments that capture receptor dynamics in intact

CXV: The Class F of G Protein-Coupled Receptors Yusman Manchanda, Dr. Molecular insights into orphan G protein-coupled receptors relevant to schizophrenia Single nucleotide variations encoding missense mutations in G protein-coupled receptors may contribute to autism GPCRs Unravelling G protein-coupled receptor signalling networks using global phosphoproteomics Reviews, GPCRs CXV: The Class F of G Protein-Coupled Receptors Structural and Molecular Insights into GPCR Function

GPCR contributor article Canonical chemokine receptors as scavenging “decoys” Shivani Sachdev, Brendan Bouvier, Jana Selent, et al. for their study on G protein-specific mechanisms in the serotonin 5-HT2A receptor function, impacting synaptic transmission Orphan receptor GPR88 as a potential therapeutic target for genome sequence analysis in India Methods & Updates in GPCR Research Engineering G protein-coupled receptors Phase 2a Obesity Study and Capsule to Tablet PK Study for its Oral Non-Peptide Small Molecule GLP-1 Receptor

G protein-coupled receptors (GPCRs) are a vast family of membrane-bound proteins crucial for transmitting These receptors typically engage specific G protein subtypes, such as Gs, Gi/o, Gq/11, and G12/13, at Using BRET based approaches, the Gs-coupled vasopressin V2 receptor (V2R) was shown to form a stable Okashah, N., et al., Agonist-induced formation of unproductive receptor-G(12) complexes.  Stallaert, W., et al., Purinergic Receptor Transactivation by the β(2)-Adrenergic Receptor Increases

Jürgen Wess and Liu Liu for their study on A novel function of the M2 muscarinic receptor Drs. Zhan-Guo Gao, Mansour Haddad, and Kenneth A Jacobson for their work on A2B adenosine receptor signaling for breast cancer GPCR Activation and Signaling The TAS1R2 G-protein-coupled receptor is an ambient Kinetic Model for the Desensitization of G Protein-Coupled Receptor RNA-seq screening and gene function variants in the hypothalamic-pituitary-gonadal axis1 A novel function of the M2 muscarinic receptor

changes to clarify the molecular mechanisms governing ligand efficacy and potency at the β2 adrenergic receptor For example, orthosteric drug design —in which drugs bind to the receptor’s primary active site—can now be optimised by targeting specific ligand-receptor interactions to modify efficacy and potency. Allosteric modulators offer a promising approach for developing drugs that enhance or inhibit receptor Molecular basis of proton-sensing by G protein-coupled receptors. bioRxiv .

Azietaku , our great contributor, for his article Class B1 GPCR Dimerization: Unveiling Its Role in Receptor variant in RGS18 candidate for a familial mild bleeding syndrome Fusarium graminearum Ste2 and Ste3 Receptors Heterodimerization when Expressed Heterologously in Saccharomyces cerevisiae The beta 2 adrenergic receptor Neuronal Precursor Cells Derived from Patients Diagnosed with Schizophrenia Sphingosine 1-phosphate receptor the CaSR gene Reviews, GPCRs, and more Insight into structural properties of viral G protein-coupled receptors

Picture this: two compounds bind to the same receptor. One sparks a firestorm of cellular activity. Terry walks you through real-world experiments, decades of receptor pharmacology wisdom, and the cutting-edge

Anderson, Sudarshan Rajagopal, Robert Lefkowitz, Howard Rockman for their review G Protein-Coupled Receptors interaction enables synergistic membrane-to-nucleus information transfer TMC6 functions as a GPCR-like receptor to sense noxious heat via Gαq signaling Exploring the Activation Mechanism of the GPR183 Receptor GPCR , Drugs, and more Target-based discovery of antagonists of the tick (Rhipicephalus microplus) kinin receptor proteins in rice (Oryza sativa) G Protein-Coupled Receptors: A Century of Research and Discovery Challenges

Can we leverage structural and computational insights not just to explain receptor–ligand interactions challenge  such as differentiating agonists from antagonists, predicting biased agonism, or achieving receptor Instead of rehashing how a known ligand binds to a known receptor, they aim to produce predictions that For dopamine receptor studies, they built predictive models before experimental structures were available It struggles with ligand-bound conformations, GPCR–G protein complexes, and receptor–peptide interactions

Celtarys Research expands its assay tools with CELT-419 for D3 receptor studies, and Dr. Terry Kenakin brings translational clarity to complex receptor concepts.   Platforms   Celtarys Research presents CELT-419, a nanomolar-affinity fluorescent ligand optimized for D3 receptor Highlights     Phosphorylation selectively regulates β-arrestin recruitment  across glucagon family receptors

Adhesion GPCRs Adhesion G Protein-Coupled Receptor Gpr126 (Adgrg6) Expression Profiling in Diseased Mouse 2 Inverse Agonists Development of Putative Bivalent Dicovalent Ligands for the Adenosine A1 Receptor in intestinal stem cells to exacerbate colitis The EBI2 receptor is coexpressed with CCR5 in CD4+ T Molecular Insights into GPCR Function Bilayer lipids modulate ligand binding to atypical chemokine receptor  3 Industry News New cannabinoid CB1 receptor antagonists disclosed in Inversago patent Orion Biotechnology

including G protein coupled receptors (GPCRs). This phenomenon has been demonstrated for receptors such as the parathyroid hormone receptor (PTHR) and the vasopressin receptor 2 (V2R). Sustained cyclic AMP production by parathyroid hormone receptor endocytosis. Persistent cAMP Signaling by Internalized LH Receptors in Ovarian Follicles.

G protein-coupled receptors (GPCRs) are major drug targets, yet their complex and dynamic structures For the σ2 receptor, AF2 predicted side-chain conformations with an RMSD of 1.1 Å from the crystal structure Docking 490 million molecules against the σ2 receptor's AF2 model yielded a 54% hit rate, comparable For the 5-HT2A receptor, AF2 models showed some variations at key residues, and docking 1.6 billion molecules Functional activity of selected compounds was assessed across 5-HT2A, 5-HT2B, and 5-HT2C receptors, with

intracellular allosteric site GPCRs represent one of the largest and most vital families of cell surface receptors distinct, often less conserved sites on the receptor. This allows for the fine-tuning of receptor activity, leading to more specific and safer drugs. Allosteric binding sites on the receptor are those topographically distinct from (do not exhibit any in their orthosteric binding sites, such as chemokine receptors.

of Tribolium castaneum GPCR Activation and Signaling Palmitoylation of the Glucagon-like Peptide-1 Receptor Modulates Cholesterol Interactions at the Receptor-Lipid Microenvironment Basal interaction of the orphan receptor GPR101 with arrestins leads to constitutive internalization Identification of G Protein-Coupled ligand efficacy and potency in GPCR signaling Activation and characterization of G protein-coupled receptors functionalized Drosophila dopamine receptors Targeting CB2R in astrocytes for Parkinson's disease therapy

and Graeme Milligan for their research on the Regulation of the pro-inflammatory G protein-coupled receptor Alejandra Tomas, et al. for their study on Lipid regulation of the glucagon receptor family Drs. is involved in the resistance of Rhopalosiphum padi to pyrethroids Discovering allatostatin type-C receptor brainstem parabrachial neurons to suppress feeding The C-terminus of the prototypical M2 muscarinic receptor family Technologies for the discovery of G protein-coupled receptor-targeting biologics Lipid mediators

Fast-forward a few thousand years, and we’re talking beta receptors, receptor theory, and AI-generated

advent of AlphaFold, homology modeling was the most common method for predicting G protein-coupled receptor cellular environment which are crucial for understanding how drugs can selectively target different receptor To fully understand GPCR behavior and optimize drug targeting across multiple receptor states, experimental Ligand discovery from a dopamine D3 receptor homology model and crystal structure. AlphaFold accelerated discovery of psychotropic agonists targeting the trace amine-associated receptor

Human cells express over 800 G-protein-coupled receptors (GPCRs) to facilitate communication with the These receptors respond to a variety of signals by undergoing structural changes that activate internal variability analysis to monitor the transitions of the Gs protein in complex with the β2-adrenergic receptor This interaction significantly increases the receptor’s affinity for GTP, allowing a detailed observation Physiological roles of G protein-coupled receptor kinases and arrestins.

One fascinating aspect of the cellular signaling network is the crosstalk between G protein-coupled receptors (GPCRs) and receptor tyrosine kinases (RTKs). The interaction between these two receptor types raises intriguing questions about how their signaling The cross-talk between growth factor receptors and GPCRs is an intriguing area of study. migration assays to investigate the effects of these modifications on key signaling events such as receptor

(GBA) motif Mechanisms of biased agonism by Gαi/o-biased stapled peptide agonists of the relaxin-3 receptor agonists at the cannabinoid CB1 receptor Why classical receptor theory, which ignores allostery, can ACKR3 GPCRs in Cardiology, Endocrinology, and Taste The Role of G Protein-Coupled Receptors and Receptor Kinases in Pancreatic β-Cell Function and Diabetes GPCRs in Neuroscience Voltage tunes mGlu5 receptor function, impacting synaptic transmission The multifaceted role of the CXC chemokines and receptors

Genomics, in turn, played a crucial role in the discovery and sequencing of the beta-adrenergic receptor Another significant impact of genomics on GPCR research is the elucidation of receptor structure and For example, we know that transmembrane helices move during receptor activation and that the DRY motif Cloning of the gene and cDNA for mammalian beta-adrenergic receptor and homology with rhodopsin. The G-protein-coupled receptors in the human genome form five main families.

Graaf, Cherine Bechara, et al. for their work on Conformational dynamics underlying atypical chemokine receptor Mancinelli, Joshua Levitz, David Eliezer, et al. for their research on Control of G protein-coupled receptor Fluorophore-Labeled Pyrrolones Targeting the Intracellular Allosteric Binding Site of the Chemokine Receptor subtypes Structural insights into ligand recognition, selectivity, and activation of bombesin receptor subtype-3 Control of G protein-coupled receptor function via membrane-interacting intrinsically disordered

18th, 2024 Adhesion GPCRs Heterogeneity of tethered agonist signaling in adhesion G protein-coupled receptors cascade Allatotropin (AT) related peptides L-ATRP and D2-ATRP diastereomers activate an endogenous receptor Binders, Drugs, and more Photo-BQCA: Positive Allosteric Modulators Enabling Optical Control of the M1 Receptor signaling in humoral immunity Methods & Updates in GPCR Research Probing PAC1 receptor activation across Application Case Study Constitutive and Conditional Epitope Tagging of Endogenous G-Protein-Coupled Receptors