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

their research on Functional consequences of spatial, temporal and ligand bias of G protein-coupled receptors Fluorescent Probes and Applications in Single-Molecule Microscopy of Wild-Type Receptors Dr. Inverse Regulation of C-C Chemokine Receptor 3 Oligomerization by Downstream Proteins Indicates Biased Signal Transduction Pathways Activation of a GPCR, ORL1 receptor: A novel therapy to prevent heart failure Fluorescent Probes and Applications in Single-Molecule Microscopy of Wild-Type Receptors Structural

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

GPCR activation typically occurs through the binding of agonists which stabilize receptor conformations The initial demonstration of spontaneous or "constitutive" receptor activity was reported for the β2- adrenergic receptor in 1984 (Cerione et al. 1984), where reconstitution of purified β2-adrenergic receptors GPCR ligands pharmacology The impact of a ligand on a receptor's structure and biophysical attributes in their orthosteric binding sites, such as chemokine receptors.

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 .

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

Analysis of Frizzled-Dishevelled Interactions Using BRET Biosensors Reveals Functional Differences among Receptor Kogut-Günthel , Antonella Di Pizio , et al. for their research on The path to the G protein-coupled receptor , new biophysical techniques, and medicinal chemistry approaches in understanding these challenging receptors in Skin Aging The path to the G protein-coupled receptor structural landscape: Major milestones and N-terminal single-nucleotide variants modulates receptor processing and functional activity Differential

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

Di Pizio, Jiafei Mao, Jana Selent, et al. for their research on the Relevance of GPCR dynamics for receptor to heterotrimeric G protein activity biosensors Descriptive molecular pharmacology of the δ opioid receptor GPCRs in Neuroscience An atlas of GPCRs in dopamine neurons: Identification of the free fatty acid receptor Pharmacology for the Treatment of Metabolic Disease Relevance of G protein-coupled receptor (GPCR) dynamics for receptor activation, signalling bias and allosteric modulation Structural and Molecular Insights

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

work on International Union of Basic and Clinical Pharmacology CXV: The Class F of G Protein-Coupled Receptors reveal a discrete cellular mechanism of endosomal G protein activation Amylin receptor subunit interactions Junction, Leading to D-CMP Steviol rebaudiosides bind to four different sites of the human sweet taste receptor Research Development of a NanoBRET Assay Platform to Detect Intracellular Ligands for the Chemokine Receptors Structural and Molecular Insights into GPCR Function Structure of endothelin ETB receptor-Gi complex

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.

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.

Kotliar , Thomas Sakmar , et al. for their study on Multiplexed mapping of the interactome of GPCRs with receptor activity-modifying proteins Molecular mechanism of bitter taste receptor agonist-mediated relaxation Urotensin II Peptide Analogues: A Proposed Key Role of the N-Terminal Region for Novel Urotensin II Receptor Modulators GPCRs in Oncology and Immunology G protein-coupled receptor-mediated signaling of immunomodulation variants and human genetic disease Advances in yeast synthetic biology for human G protein-coupled receptor

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

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

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

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.

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

Enhanced Drug Discovery Cam Sinh Lu GPCR-BSD: a database of binding sites of human G-protein coupled receptors partner on GPCRs Nxera Pharma’s Partner Centessa Initiates Phase 2 Trial with ORX750, a Novel Orexin Receptor Chemistry GPCR Activation and Signaling Pathophysiological significance and modulation of the transient receptor canonical 3 ion channel Smad transcription factors as mediators of 7 transmembrane G protein-coupled receptor signalling The voltage sensitivity of G-protein coupled receptors: Unraveling molecular mechanisms and

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

, Joshua Levitz for their work on Emerging modes of regulation of neuromodulatory G protein-coupled receptors GPCR Activation and Signaling Emerging modes of regulation of neuromodulatory G protein-coupled receptors adult male mice Methods & Updates in GPCR Research RNA therapeutics in targeting G protein-coupled receptors challenges Structural and Molecular Insights into GPCR Function Structural perspectives on chemokine receptors Pharmacology 2026 GPCR Jobs HIGHLIGHT Principal Scientist, In vitro pharmacology Senior Scientist - Receptor

Canonical chemokine receptors – scavenging “decoys” Chemokine receptors coordinate cell migration upon Upon activation, chemokine receptors coupe to the Gαi class of heterotrimeric G proteins, which, in turn The chemokine receptor family comprises 19 canonical chemokine receptors together with 4 atypical chemokine C terminus by G protein receptor kinases (GRKs), specifically GRK2 and GRK3 (A. But why do canonical chemokine receptors have this dual role in physiology?

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.

Tagged for arrest: 'Barcode' determines receptor's fate. Our next Dr. Molecular insights into peptide agonist engagement with the PTH receptor. How can we improve the measurement of receptor signaling bias? New paradigms in purinergic receptor ligand discovery. The role of G protein conformation in receptor-G protein selectivity.

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

endocytic and secretory pathways via MADD, a Rab11A effector that activates Rab27B Targeting of insulin receptor Binding Studies for the Orphan Class A GPCR GPR3 Antimalarial and Plasmodium falciparum serpentine receptor 12 targeting effect of FDA approved purinergic receptor antagonist GPCRs in Cardiology, Endocrinology Signaling Optical Approaches for Investigating Neuromodulation and G Protein-Coupled Receptor Signaling Protocol for identifying physiologically relevant binding proteins of G-protein-coupled receptors Reviews