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contributor, for his article Class B1 GPCR Dimerization: Unveiling Its Role in Receptor Function and Signaling Scientist/Staff Scientist, Computational Chemistry Postdoc in GPCR mechanosensing   GPCR Activation and Signaling adrenergic receptor cross-linked interactome identifies 14-3-3 proteins as regulating the availability of signaling-competent receptors GPCRs in Neuroscience Astrocyte Gi-GPCR signaling corrects compulsive-like grooming and anxiety-related Neurodegenerative Disorders: Integrating Structural Biology and Drug Discovery Approaches Altered PLCβ/IP3/Ca2+ Signaling

Breakthroughs this week:  Potentiation of GPCR signaling by ATP and sugar monophosphates; Pharmacology GPCR Premium: Sneak Peek Here’s a curated, high-signal preview of what Premium Members get this week—no Plus: top tracks to watch at GPCR Forum 2025, fresh postdoc openings at the ADME/signaling interface If you care about compartmentalized signaling and native-state biology, this is a sharp, readable tour Why micro-domains change what “global” signaling can and can’t explain.

G protein-coupled receptor signaling analysis using homogenous time-resolved Förster resonance energy This makes it an ideal candidate for GPCR research, where accuracy in detecting subtle signaling changes Signal interferences are kept to a minimum thanks to the timing of detection. Quite often, there is a need to amplify the signal  strength to detect them, which can be achieved by G protein-coupled receptor signaling analysis using homogenous time-resolved Förster resonance energy

GPCR signaling almost never follows a straight path. balancing opposing forces—vasoconstriction vs. vasodilation, sympathetic vs. parasympathetic tone, signal In this module, you’ll explore how some receptor–agonist complexes continue signaling from endosomes, creating “protected” signaling that extracellular antagonists can’t block. You’ll come away asking Which of my ligands might be producing hidden signaling from inside the cell—and

The work introduced him to hormonal signaling, appetite regulation, and cellular communication systems Receptor localization, ligand access, and intracellular signaling can look different in actual tissues It affected hormone signaling between alpha and beta cells, but the mechanism was unclear. and structural studies revealed that this protein was interacting with GPCRs involved in metabolic signaling GPCR–islet signaling links extended beyond classical ligand models.Collaboration and long-term persistence

Crecelius , Sara Benzow , Adriano Marchese Cannabinoid regulation of angiotensin II-induced calcium signaling , Ana Rodríguez-Pérez , Gemma Navarro , José Labandeira-García , Rafael Franco Endomembrane GPCR signaling Petrovic , Stephan Grzesiek , Polina Isaikina NMR spectroscopy reveals insights into mechanisms of GPCR signaling /Structural Biologist Senior Scientist/Staff Scientist, Computational Chemistry GPCR Activation and Signaling in striatal neurons Receptor-dependent influence of R7 RGS proteins on neuronal GIRK channel signaling

For targets such as CB2, where nuanced shifts in receptor conformation affect signaling outcomes, a whole-cell decisions Why Live-cell High-Content Screening Matters for CB2 Ligand Profiling CB2 is a GPCR whose signaling morphological changes at this concentration, supporting the interpretation that reductions in tracer signal A progressive reduction in tracer signal is observed at higher concentrations, consistent with competitive As the field moves toward more nuanced understandings of CB2 signaling, tools that preserve cellular

Biased agonism is a phenomenon where different ligands acting on the same receptor trigger distinct signaling revealing that different ligands can stabilize distinct receptor conformations, leading to diverse signaling These differences in signaling profiles can have significant physiological implications. Christopoulos, Signalling bias in new drug discovery: detection, quantification and therapeutic impact AZIETAKU, J.T., Profiling Glucagon-Like Peptide -1 Receptor Transducer Coupling, Signalling and Biased

GPCR, we’re decoding arrestin-driven signaling and spotlighting the tools to match.   NTSR1 modulator targets pain without the need for opioids, and a real-time lipid probe tracks early signaling Terry Kenakin, these five modules reveal how location bias, intracellular signaling, and ligand kinetics

With nanomolar affinity, high specificity, and a strong signal-to-noise profile, this non-radioactive Decoding PTH1R Gq Signaling Cryo-EM structures of Gq-bound PTH1R uncover glycan and loop-based mechanisms shaping G-protein preference, offering a path toward signaling-biased osteoporosis therapies.   how two ligands differently activate class A GPCR NMBR, with allosteric communication hubs modulating signaling

your career or pushing the edge of MoA design, weekly lesson help you apply key concepts like binding, signaling With strong signal stability, HTS compatibility, and broad assay versatility, CELT-419 is designed for   show both driver-like patterns and high redundancy, prompting a call for multiomics to distinguish signal CXCR4 oligomerization  sustains oncogenic signaling in lymphoid neoplasms, and its disruption boosts

By the time his lab began dissecting the GLP-1 and GIP receptor landscape in islets and brain, the signal GPCR signaling wasn’t linear. It wasn’t clean. It fused them, creating a hybrid view of receptor signaling that has now been adopted by labs worldwide The signaling didn’t line up. The knockout behaved differently than expected. It will hinge on the teams who can map GPCR signaling with precision and design therapies that fit real

Breakthroughs this week: Decoding ADGRE5 signaling; Eli Lilly’s obesity pill vs Novo’s Wegovy; Certa and Novo Upcoming events:  September GPCR symposia across Europe, UK, and online—including neuroGPCR signaling Must-read publications:  Tryptophan-cholic acid and MRGPRE in glucose homeostasis; Biased signaling in With Premium, you move faster, smarter, and more confidently than peers relying on scattered signals. Those who act on the right signals today will lead tomorrow’s breakthroughs—and avoid delays others won

protein species itself ✅ Real-world case studies showing binding-function dissociation and residual signal It redefines how we interpret radioligand curves , shifts in signal, and the meaning of “inhibition.” Kenakin shows how even small cooperativity values (like α = 0.1) cap the shift in signal . ) β:  Dual cooperativity—how ternary complexes influence each other This framework explains partial signals irreversibility, but because there isn’t enough G protein in the system to form the species that would lower the signal

👉 Why has intellectual property become a first-order fundraising signal? intellectual property is no longer something that comes up late in the process. 👉 It has become an early signal It signals whether the company has thought through scale, competition, and control.   When that signal is weak or confusing, investors slow down. It is a signal of how well you understand your own company. Ready to Break Your Bottlenecks?

Broichhagen aka JB, the goal was bold and elegant: Create a photo-switchable ligand to remotely control GPCR signaling The idea was simple — turn signaling on or off with a flash of light. Except: Nothing behaved. This solved a long-standing problem in GPCR biology: You can't understand signaling if you can’t see  GPCR localization relied on: Antibodies of inconsistent specificity Fixed tissue sections Indirect signaling

Must-read publications:  Stay updated on cutting-edge research, including the potentiation of GPCR signaling Catherine’s research, blending GPCR signaling studies with public health data, offers critical insights intersect—and why pharmacologists are critical in addressing this crisis ➤ Call for Papers – GPCRs: Signal Transduction Volume II With over 21,000 views  and 7,785 downloads  from Volume I, the Signal Transduction Those who act on the right signals today will lead tomorrow’s breakthroughs—and avoid delays others won

Breakthroughs this week: FFA4 receptor signaling controls lipolysis at lipid droplets; novel atypical Upcoming events:  An exclusive preview of the “neuroGPCR: G protein coupled receptor signaling in its Must-read publications:  New insights on RGS protein modulation, GRK2-biased β₂AR signaling, and the Gain a competitive edge by staying on top of the latest breakthroughs in allostery, biased signaling, Those acting on the right signals today will shape tomorrow’s breakthroughs—and avoid delays others won

GPCR Symposia Our upcoming symposium on March 15th is about GPCR activation and signaling. GPCR signaling bias: an emerging framework for opioid drug development Structural and functional insight pathway The non-nutritive sweetener sucralose increases β-arrestin signaling at the constitutively active orphan G protein-coupled receptor GPR52 Endosome positioning coordinates spatially selective GPCR signaling GRK5 promoted renal fibrosis via HDAC5/Smad3 signaling pathway Non-canonical G protein signaling GPCR

contributor, for his article Class B1 GPCR Dimerization: Unveiling Its Role in Receptor Function and Signaling the Year at the Citeline Japan Awards 2024 GPCR therapies: Eight promising biotechs hacking the cell signaling /Structural Biologist Senior Scientist/Staff Scientist, Computational Chemistry GPCR Activation and Signaling receptors GPCRs in Neuroscience Astrocyte Gi-GPCR signaling corrects compulsive-like grooming and anxiety-related Neurodegenerative Disorders: Integrating Structural Biology and Drug Discovery Approaches Altered PLCβ/IP3/Ca2+ Signaling

These challenges can obscure real biological signals and complicate the identification of robust hits well-suited for GPCR research, where receptor trafficking, spatial dynamics, and context-dependent signaling Key limitations of radioligand assays include:  • No spatial information  — signals are measured in bulk Imaging Calibration and Acquisition These steps ensure that quantitative signals reflect biology, not -expressing HEK cells, the fluorescent ligand CELT-331  produces precise membrane-localized binding signals

of the largest and most vital families of cell surface receptors, playing a pivotal role in cellular signaling and chemokine signaling, extending to numerous other GPCR-regulated systems such as free fatty acid Allosteric agonists binding to intracellular sites can also promote G-protein signaling. Advances in understanding the structural and mechanistic aspects of biased GPCR signaling are crucial This site allows for the direct modulation of downstream receptor signaling in an allosteric manner.

Gutkind, Edward C Stites, et al., for their study on Systems modeling of oncogenic G-protein and GPCR signaling New ligands and new GPCR behaviors that produce unique drug profiles (i.e., intracellular ligands and signaling , location bias, signaling bias). dynamics underlying atypical chemokine receptor 3 activation RhoA-mediated G12-G13 signaling maintains muscle stem cell quiescence and prevents stem cell loss Activation of Polycystin-1 Signaling by Binding

in adhesion G protein-coupled receptors GPCR Activation and Signaling A-Kinase-Anchoring-Protein Subtypes Differentially Regulate GPCR Signaling and Function in Human Airway Smooth Muscle GRK2 kinases in the primary cilium initiate SMOOTHENED-PKA signaling in the Hedgehog cascade Allatotropin (AT) related peptides the glucagon subfamily of GPCRs GPCRs in Cardiology, Endocrinology, and Taste Regulator of G-protein signaling neuroprotective and neurogenic properties GPCRs in Oncology and Immunology Chemoattractant receptor signaling

Confocal Imaging of GPCRs: From Live to Fixed Cells GPCRs are present across cell membranes transmitting signals their dynamics in both a spatial and temporal manner is key to understanding how they work in this signaling one of the best used of confocal microscopy is the study of receptor trafficking, localization and signaling Right panel, the fluorescent signal is displaced when, after incubating with CELT-327, cells are incubated

Robert Lefkowitz for their work on GPCRs: from radioligand binding to cellular signaling Dr. Next week, on March 15th, we are hosting a symposium on GPCR activation and signaling. via single amino acid substitution G protein-coupled receptors: from radioligand binding to cellular signaling Bicarbonate signalling via G protein-coupled receptor regulates ischaemia-reperfusion injury GPCRs in pathway Blockade of vasoactive intestinal peptide receptor 2 (VIPR2) signaling suppresses cyclin D1-

Why This Matters GPCR research demands integration — pharmacology, structural biology, signaling pathways What Happens When Labs Stop Competing Michelle credits this environment for catalyzing the GPCR signaling Model Evolved Year 0  — Shared lab space established; PI buy-in secured Year 2  — Core imaging and signaling It’s a competitive advantage. 🎧 Listen to the full episode:   Leadership, Luck, and GPCR Signaling 🔓

It’s a curated lens—just enough signal to guide your week, with the full depth available inside. compatibility, and higher specificity enable real-time tracking of interactions, internalization, and biased signaling—without Eliminate fix/perm distortions:  Preserve receptor conformation and downstream signaling integrity. experiments, or time a move in the market or your career, Premium makes sure you’re working from the clearest signal Those acting on the right signals today will shape tomorrow’s breakthroughs—and avoid delays others won

It was the result of chemistry, collaboration, and relentless effort until the signal finally confirmed and have a longer lifespan as internalized receptors enter acidic endosomes—translating biology into signal Rare-earth probe synthesis begins Collaborative screening of scaffold families Key milestone: Clean signal Teams are already investigating temperature effects, biased signaling, and endogenous dynamics.

between extracellular and transmembrane domains modulates holo-adhesion GPCR function GPCR Activation and Signaling P2X7R-primed keratinocytes are susceptible to apoptosis via GPCR-Gβγ-pERK signal pathways Chemogenetic engagement of different GPCR signaling pathways segregates the orexigenic activity from the control parathyroid hormone-GPCR-arrestin complex Myosin VI drives arrestin-independent internalization and signaling Ultrastructure and transcriptional profile Adult single-nucleus neuronal transcriptomes of insulin signaling