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- 📰 GPCR Buzz: August 5-11, 2024 | Top Highlights from DrGPCR University!
Dates: October 3 to 31, 2024 What You’ll Master during the five sessions: Utilizing new cellular assays Alzheimer's disease Nanoplastic at environmentally relevant concentrations induces toxicity across multiple GPCR-RAMP complexes with MolBoolean Screening GPR75 Modulators Using Medium-Throughput Reporter Gene Assay 4th Transatlantic ECI GPCR Symposium September 18, 2024 | FREE Webinar - The value of GPCR cell-based assays
- Why “Displacement” Misleads You: Allosteric Binding Demystified
If you’re applying orthosteric logic to modulator-driven systems, you’re likely misreading your assays—and Binding assays report on one set of receptor states. Functional assays track another.
- Extracellular signal-regulated kinases – a potential pathway for GPCR-targeted drug discovery
This emphasis may have caused other signaling pathways to be overlooked due to a need for adequate assay This further underscores the need for advanced assay technologies and a deep understanding of cellular Recently, several high-throughput screening (HTS) assays for ERK activation have been developed, each Each assay offers unique advantages for detecting ERK activation, contributing to the broader toolkit By understanding the intricacies of GPCR signaling and utilising advanced assay technologies, researchers
- How to Use Statistical Methods to Strengthen Every GPCR Drug Discovery Decision
opportunities: Leadership-level roles in clinical operations and translational science, alongside multiple validate differences, confirm subtle shifts, and benchmark your results against literature or across assay Validate with confidence: Benchmark your results against literature standards and confirm whether your assays
- Is Your Agonist Really “Working”—Or Are You Just Seeing What Your System Allows?
analogies (think batteries and balance scales), Terry reveals why different tissues—and even different assays—can
- Pharmacology Isn't What You Think—It's So Much More
Whether you're heading into your first assay or trying to make sense of inconsistent data, Terry gives
- A NanoBRET-Based H 3 R Conformational Biosensor to Study Real-Time H 3 Receptor Pharmacology in...
activation state of G protein-coupled receptors are a useful addition to the molecular pharmacology assay the detection of both (partial) agonism and inverse agonism on living cells in a microplate reader assay better correlated with binding affinity values that were measured in radioligand competition binding assays biosensor in membranes might be a ready-to-use, high-throughput alternative for radioligand binding assays that in addition can also detect ligand efficacies with comparable values as the intact cell assay."
- Predicting GPCR Function: Inside the Carlsson Lab’s Modeling Toolbox
Every computational hypothesis moves downstream into experimental assays via close collaborations. Fast forward to today: dozens of GPCR structures exist, many in multiple conformations or bound to G Matters Now The convergence of machine learning, improved GPCR structures, and scalable experimental assays
- Maria’s Travel Blogs: ACSMEDI-EFMC Medicinal Chemistry Frontiers 2025
After all, a good tool makes a good assay, and a good assay improves research capacity.
- Decoding Schild Analysis: The Pharmacologist’s Lens on Competitive Antagonism
Some responses—especially in calcium assays or complex tissue systems—depress the maximum agonist effect Calcium flux assays, though tricky, yield valid Schild plots when analysis excludes non-equilibrium maxima Caveat: Without multiple concentrations, competitive nature remains an assumption. pA₂ is an elegant
- Isoform-and ligand-specific modulation of adhesion GPCR ADGRL3/Latrophilin3 by a synthetic binder
protein-coupled receptors (aGPCRs) are cell-surface proteins with large extracellular regions that bind to multiple In cellular-adhesion assays, LK30 specifically broke the trans-cellular interaction of ADGRL3 with teneurin
- Orthosteric vs. Allosteric Interactions: The Silent Decider of Safety and Success
Kenakin walks through this as a living system , showing how GPCRs exist in multiple conformations and This has immediate implications for interpreting EC50 shifts, partial agonism, and assay readouts—especially The result is not just cleaner assay design but a sharper decision framework for selecting, prioritizing
- Unlocking the Therapeutic Potential of Previously Undruggable GPCRs
activity (receptor binding affinity, G protein and arrestin signaling) in high throughput cell-based assays considerably more potent than the leading small molecule competitors in in vitro functional inhibition assays Figure 5: In an in vitro functional signaling assay on a human monocytic cell line, OB-004 demonstrated Figure 6: In a flow-based human monocyte endothelial transmigration assay, OB-004 strongly outperformed rapidly synthesize candidate hits from library-based screening so that they can be tested in cell-based assays
- Unlock the Future of GPCR Science: Breakthroughs and Courses Await | Sep 2 - Sep 8, 2024
for their work on The N terminus-only (trans) function of the Adhesion GPCR Latrophilin-1 controls multiple Topics: New cellular assays, real-time kinetics, and unique GPCR behaviors. 🔥 Why You Should Enroll Engaging multiple sclerosis by drugging a “simple” GPCR. 4th Transatlantic ECI GPCR Symposium September 18, 2024 | FREE Webinar - The value of GPCR cell-based assays position Adhesion GPCRs The N terminus-only (trans) function of the Adhesion GPCR Latrophilin-1 controls multiple
- Mechanism vs. Assumption: A Model-First Path to Getting GPCR MoA Right
to replace inference with models that disentangle mechanism—so your next go/no-go, dose range, and assay Engineer assays on purpose: Set ranges, controls, and system sensitivity to surface mechanism—before Assay flexibility: Combine self-labeling tags with quantitative readouts (e.g., TR-FRET) to expand mechanism
- Why Sokhom Pin Never Left GPCRs, Even When Everyone Else Did
While others pivoted, Sokhom went deeper: refining assays, exploring signaling bias, and building a robust
- GPCR Happy Hour – Boston, Sept 2025
Leveraging decades of experience, their services include AI-driven target identification, target validation, assay platform, iPSC-derived models, optogenetics, and high-content screening techniques such as cell painting assays
- 📰 GPCR Weekly Buzz: Exciting Schedule Shifts for Principles of Pharmacology I & II | August 12-18, 2024
Dates: October 31, November 7 - 14 -21, and December 5, 2024 (five sessions) Topics: New cellular assays to promote morning wakefulness LPA3 agonist-producing Bacillus velezensis ADS024 is efficacious in multiple 4th Transatlantic ECI GPCR Symposium September 18, 2024 | FREE Webinar - The value of GPCR cell-based assays
- Delineation of GPR15 receptor-mediated Gα protein signaling profile in recombinant mammalian cell
compounds to delineate the GPR15 receptor-mediated Gα protein signalling using a G protein activation assay and second messenger assay conducted on living cells. results show that the GPR15 receptor preferentially couples to Gi/o rather than other pathways in both assays
- Understanding Enzyme Inhibition In GPCR Discovery Programs
Whether you’re building assays or a scientific career, this is a must-read on why risk, surprise, and Biosensors make once-invisible dynamics assayable at scale. Read the roundup ➤ Why Dr.
- Lab Leadership Without Ego: How Sokhom Pin Built the Happiest Team at Alkermes
tasked with building an in vitro pharmacology group from scratch , including infrastructure, hiring, assay
- G protein-coupled receptor 21 in macrophages: An in vitro study
expression was evaluated at gene and protein level, the signalling pathway was investigated by an IP1 assay Cell migration was detected by the Boyden chamber migration assay, performed on macrophages derived from
- Applications of Fluorescent Probes in Confocal Imaging of GPCRs: From Live to Fixed Cells
other ligands and are very interesting in TR-FRET (Time-Resolved Förster Energy Resonance Transfer) assays A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery.
- GPCR Allosteric Modulation: Why Allostery is the Engine of Drug Discovery
Cryptic Sites, Longer Onset: Why Some Drugs Work Differently in Cells Than in Assays One of the most This has direct implications for: Assay timing and readout design Misclassification of lead candidates
- From Failed Experiments to Predictive GPCR Models
Watch Episode 175 From failed assays to breakthroughs in GPCR modeling , Dr. Carlsson notes that it’s easier to find pharmacologists to run assays than it is to persuade chemists Trainees must learn how to interpret assay data, understand pharmacological context, and communicate
- How Schild Analysis Protects Your Conclusions in GPCR Research
Terry’s Corner: Schild Analysis — Why It Matters Most assays show a clean rightward shift and we assume Who should listen Researchers navigating complex datasets, balancing innovation with assay rigor, or
- The Adhesion GPCR VLGR1/ADGRV1 Regulates the Ca2+ Homeostasis at Mitochondria-Associated ER Membrane
We confirmed the interaction of VLGR1 with key proteins of MAMs by pull-down assays in vitro complemented by in situ proximity ligation assays in cells.
- 📢 GPCR Update: August 19-25, 2024 | Thrilling Announcement: New Pharmacology Course Dates & Exclusive Discounts Inside!
Topics cover new cellular assays, real-time kinetics, and unique GPCR behaviors. 4th Transatlantic ECI GPCR Symposium September 18, 2024 | FREE Webinar - The value of GPCR cell-based assays
- CCL25/CCR9 interaction promotes the malignant behavior of salivary adenoid cystic carcinoma via...
8 and colon formation, and cell migration and invasion were detected by wound healing and transwell assays Western blot and RT–qPCR assays were carried out to measure the downstream factors of the interaction
- Ben Clements on Rescuing Opioids with GPCR Modulators
mu-opioid receptor, positive allosteric modulators, GPCR training program, GPCR online course, GTPγS assay























