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- From Failed Experiments to Predictive GPCR Models
With limited structural data but a growing pharmacological interest, GPCRs presented the perfect challenge Pharmacology, on the other hand, is often outsourced through collaborations with expert labs who specialize 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 predictive modeling matures, its role will continue to expand, guiding ligand discovery, informing pharmacology
- Curve Shifts Don’t Lie, But Your Eyes Might
When Curves Shift Some of the most difficult calls in pharmacology happen when two curves look slightly Is it a real pharmacological effect, or just noise? Here’s where the F-test becomes indispensable. engagement opportunities through AMAs and topic suggestions Practical insights distilled from decades of pharmacology curvecomparison #ftest #assayvalidation #experimentaldesignstatistics #assayreproducibility #ANCOVA #pharmacology
- How System-Level GPCR Thinking Prevents Discovery Failures
If your work touches GPCR pharmacology, these insights aren’t optional—they’re essential. Career opportunities: Senior/Principal Scientist—GPCR Pharmacology; Principal Scientist—In Vitro Pharmacology Terry’s Corner: GPCR Pharmacology Insights That Prevent Real Drug Discovery Failures Discovery collapses Johannes Broichhagen explains how next-generation fluorescent probes—designed with precise synthetic Researchers, pharmacologists, biotech teams, and decision-makers who rely on accurate, efficient, interpretation-first
- Dr. GPCR and Eurofins DiscoverX Join Forces to Accelerate GPCR Drug Discovery
community by expanding access to validated, industry-standard GPCR assay platforms that enable rigorous pharmacological accelerate GPCR-targeted drug discovery by connecting scientists with proven assay platforms, deep pharmacological are trusted by leading pharmaceutical companies worldwide to generate high-quality, decision-enabling pharmacological
- GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between ...
GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between Health and Disease GPCRs arguably represent the most effective current therapeutic targets for a plethora of diseases. GPCRs also possess a pivotal role in the regulation of the physiological balance between healthy and pathological conditions; thus, their importance in systems biology cannot be underestimated. The molecular diversity of GPCR signaling systems is likely to be closely associated with disease-associated changes in organismal tissue complexity and compartmentalization, thus enabling a nuanced GPCR-based capacity to interdict multiple disease pathomechanisms at a systemic level. GPCRs have been long considered as controllers of communication between tissues and cells. This communication involves the ligand-mediated control of cell surface receptors that then direct their stimuli to impact cell physiology. Given the tremendous success of GPCRs as therapeutic targets, considerable focus has been placed on the ability of these therapeutics to modulate diseases by acting at cell surface receptors. In the past decade, however, attention has focused upon how stable multiprotein GPCR superstructures, termed receptorsomes, both at the cell surface membrane and in the intracellular domain dictate and condition long-term GPCR activities associated with the regulation of protein expression patterns, cellular stress responses and DNA integrity management. The ability of these receptorsomes (often in the absence of typical cell surface ligands) to control complex cellular activities implicates them as key controllers of the functional balance between health and disease. A greater understanding of this function of GPCRs is likely to significantly augment our ability to further employ these proteins in a multitude of diseases. Read full article
- Orthosteric vs Allosteric Interactions— and the pHSense Shift in Internalization
Each week we highlight the decisions that move GPCR projects forward—from pharmacology essentials to Years of chemistry, photophysics, and pharmacology condensed into one breakthrough: pHSense , a reagent They translated a fundamental principle of chemistry into a usable platform for pharmacology—showing how persistence, precision, and the courage to take on “impossible” chemistry can shift the entire GPCR receptor localization and real-time signaling shape therapeutic outcomes, fluorescent ligands deliver both precision
- The Truth About GPCR Product Launches: Years in the Making
GPCR internalization isn’t just a trafficking readout—it’s pharmacology. s partnership with Durham (chemistry) and the Institute of Functional Genomics in Montpellier (GPCR pharmacology
- Signals in Motion: Pain, Metabolism & Terry’s Corner
It will bridge foundational receptor theory with today’s most pressing pharmacological questions, from emerges as a high-potential pain target ST171, a biased 5‑HT1A agonist, delivers selective pain relief in preclinical gives you timeless and timely tools to improve selectivity, model efficacy, and design smarter GPCR pharmacology This novel agonist activates Gi/o selectively , avoiding β-arrestin and showing strong pain relief in preclinical
- New Tools, Smart Signals, and The Kenakin Brief
Early Access and Updates Terry’s Corner is launching soon with monthly courses, AMAs, and real-world pharmacology
- The Quiet Power of RGS Proteins: Rethinking Pain Pathways through GPCR Biology
And this is a recovery that is very rare to see at the preclinical level. " Such recovery is rare in preclinical pain models and hints that RGS proteins could modulate pain chronification itself . the core mediator — demonstrating the reach of these signaling pathways beyond classical receptor pharmacology
- How Understanding Intracellular Drug Access Can Transform Your GPCR Drug Discovery Program
research position in GPCR biochemistry and biophysics and a research associate/scientist in in vitro pharmacology “The best pharmacology teacher (Dr. Also super-valuable for those of us learning how to teach pharmacology” — Dr. GPCR scientists, translational pharmacologists, biotech drug discovery teams, and decision-makers who
- Developing the Cannabinoid Receptor 2 (CB2) pharmacopoeia: past, present, and future
Promising preclinical data supports the applicability of CB2 activation in autoimmune and inflammatory available, which has led to considerable advancements in the understanding of CB2 function and extensive preclinical development and progress in optimising physicochemical properties, understanding advanced molecular pharmacology
- Developing the Cannabinoid Receptor 2 (CB2) pharmacopeia: past, present, and future
Promising preclinical data support the applicability of CB2 activation in autoimmune and inflammatory available, which has led to considerable advancements in the understanding of CB2 function and extensive preclinical development and progress in optimizing physicochemical properties, understanding advanced molecular pharmacology
- Precise druggability of the PTH type 1 receptor
This study provides a computational pipeline to detect precise druggable sites and identify allosteric
- Rescue of Cell Surface Expression and Signaling of Mutant Follicle-Stimulating Hormone Receptors
Pharmacological chaperones are cell-permeant small molecules that engage nascent mutant GPCRs in the Therefore, CAN1404 acts as a pharmacological chaperone and can rescue cell surface expression and function effects of genetic mutations on GPCR function and provide a proof of therapeutic principle for FSHR pharmacological
- Differences across sexes on head-twitch behavior and 5-HT2A receptor signaling in C57BL/6J mice
Much of the understanding of psychedelic pharmacology is derived from rodent models, but most of this preclinical research has only focused on male mice. agonist DOI in C57BL/6J mice, and support the importance of studying sex as a biological variable in preclinical
- The Imprecision Problem: Why Your GPCR Drug Discovery Program Is Off-Track Before It Even Starts
Unlocking the Puzzle: The Importance of Precision in GPCR Programs and the Hidden Costs of Overlooking But because the program is run on duct tape and heroics instead of precision. It’s the absence of operational precision. Even flawless experiments collapse under sloppy systems. It’s a deliberate blueprint for precision. This doesn’t mean an overnight overhaul. If you want your program to survive, you need a Blueprint for Precision. Not next quarter.
- 📰 GPCR Weekly News, May 20 to 26, 2024
GPCR University workshop on Advanced Data Analysis for GPCR Pharmacology, led by the esteemed Dr. GPCR Matchmaking Read Mark's job spotlight article for a Principal Scientist in In Vitro Pharmacology Mark recently discussed this exciting opportunity with Beth Fleck, Director of In Vitro Pharmacology Orion Biotechnology will be attending BIO 2024 Antiverse is attending BIO 2024 Septerna to Present Preclinical 2026 GPCR Jobs HIGHLIGHT Principal Scientist, In vitro pharmacology NEW Senior Scientist - Receptor
- 📰 GPCR Weekly News, July 1 to 7, 2024
Gunnar Schulte for his study on the International Union of Basic and Clinical Pharmacology. Jianming Han, Tao Che for their analysis of GPCR-G protein selectivity revealed by structural pharmacology Here’s a sneak peek at what you can expect: Principles of Pharmacology in Drug Discovery I - Techniques Principles of Pharmacology in Drug Discovery II - Advanced Methods for the Optimization of Candidate contribute to autism GPCRs in Oncology and Immunology Emerging GPCR targets for AUD: Insights from preclinical
- FDA Approval Is a Strategy Obstacle, Not a Paperwork Problem
A solid preclinical package, promising safety data, and a consistent in vivo proof-of-concept, it feels optimizing for, and where most early-stage teams fall short: 1️⃣ Predictable safety margins: Can your preclinical Then you work upstream to define what your preclinical and early clinical data must demonstrate. practice: You align trial endpoints with future label claims , not just scientific curiosity You design preclinical
- GPCR Weekly Whirlwind: Top Receptor Highlights from Sep 30 - Oct 6, 2024!
I We are diving into the second class of our Principles of Pharmacology I course with enthusiasm and Seize this opportunity to enhance your expertise and proficiency in pharmacology! Modules: October 31st : The Eyes to See- The Importance of Pharmacologic Assays. as Chief Medical Officer and President of Nxera Pharma Japan Septerna files for IPO on strength of preclinical Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and
- Early Safety Assays: Identifying Showstoppers in GPCR Drug Discovery Pipelines Early
design cycles Computational prediction complements biological screening Why Terry’s Corner Terry’s Pharmacology focused on sharpening discovery fundamentals, challenging entrenched assumptions, and strengthening preclinical As GPCR science and pharmacological innovation accelerate, timely guidance from foundational to advanced
- 📰 GPCR Weekly News, June 3 to June 9, 2024
Congenital Adrenal Hyperplasia (CAH) and ACTH-Dependent Cushing’s Syndrome (ADCS) Septerna Presents Preclinical , 2024 | 11th Adhesion GPCR Workshop July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology 2026 GPCR Jobs HIGHLIGHT Principal Scientist, In vitro pharmacology Senior Scientist - Receptor Pharmacology Postdoctoral Scientist Senior Research Associate/Associate Scientist, Protein Science Post-Doctoral Fellow—Pharmacology
- 📰 GPCR Weekly News, May 13 to 19, 2024
GPCR University We launched the Dr.GPCR University workshop on Advanced Data Analysis for GPCR Pharmacology And don’t miss our job opportunity spotlight for a Principal Scientist in In Vitro Pharmacology! Mark discussed this position with Beth Fleck, Director of In Vitro Pharmacology at Crinetics Pharmaceuticals Ib results for its dual GLP-1/GIP receptor agonist CT-388 in people with obesity Septerna to Present Preclinical Scientist, Protein Science NEW Post-Doctoral Fellow—Pharmacology/Cell Biology/Biochemistry Post Doctoral
- 📰 GPCR Weekly News, February 6 to 12, 2023
GPCR Binders, Drugs, and more An antibody-drug conjugate targeting GPR56 demonstrates efficacy in preclinical (June 4 - 8, 2023). 2023 Molecular Pharmacology (GRS) Seminar GRC. (June 10 - 11, 2023). (June 11 - 16, 2023). 19th World Congress of Basic & Clinical Pharmacology 2023. development PhD student at Department of Drug Design and Pharmacology Software / database development postdoc at the Department of Drug Design and Pharmacology Postdoc in Bioinformatics/Data Science at
- Actions of Parathyroid Hormone Ligand Analogues in Humanized PTH1R Knockin Mice
evaluate parathyroid hormone (PTH) and PTH-related protein (PTHrP) ligands and analogues for their pharmacologic This introduces an element of uncertainty in the accuracy of rodent models for performing such preclinical
- 📰 GPCR Weekly News, April 17 to 23, 2023
Industry News Data Presented at AACR 2023 Highlights Exscientia’s Clinical and Preclinical Development GPCR Events, Meetings, and Webinars ASPET 2023 - American Society for Pharmacology and Experimental Therapeutics (June 4 - 8, 2023). 2023 Molecular Pharmacology (GRS) Seminar GRC. (June 10 - 11, 2023). Adrenoceptors and GPCR Signalling (June 30 - July 1, 2023) 19th World Congress of Basic & Clinical Pharmacology
- The Perils and Guardrails of Modifying Signalling Proteins in Bioassays
findings suggest that GPCR biosensors consisting of modified G proteins, which have been implemented in pharmacological In: Kenakin TP, editor A Pharmacology Primer (Sixth Edition). Trends in Pharmacological Sciences. 30. The mass action equation in pharmacology. Br J Clin Pharmacol. 2016;81(1):41-51. 32. Quantitative approaches for studying G protein-coupled receptor signalling and pharmacology.
- 📰 GPCR Weekly News, June 17 to 23, 2024
with Avrobio Addex Pharma unveils new mGlu7 receptor negative allosteric modulators Trevena Announces Preclinical , 2024 | 11th Adhesion GPCR Workshop July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology 2026 GPCR Jobs HIGHLIGHT Principal Scientist, In vitro pharmacology NEW Post-Doctoral Scientist- Molecular Pharmacology (FDE) NEW Research Assistant Senior Scientist - Receptor Pharmacology Postdoctoral Scientist Senior Research Associate/Associate Scientist, Protein Science Post-Doctoral Fellow—Pharmacology/Cell
- 📰 GPCR Weekly News, May 27 to June 2, 2024
Milestone Payments from Centessa Pharmaceuticals CB1 receptor inverse agonist improves lung functioning in preclinical , 2024 | 11th Adhesion GPCR Workshop July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology 2026 GPCR Jobs HIGHLIGHT Principal Scientist, In vitro pharmacology Senior Scientist - Receptor Pharmacology PostDoctoral Scientist Senior Research Associate/Associate Scientist, Protein Science Post-Doctoral Fellow—Pharmacology

















