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Career opportunities:  Principal Scientist - In Vitro Pharmacology; Senior Scientist, Molecular Pharmacology Weekly News : jobs, events, papers, industry updates Exclusive discounts on Terry’s Corner  digital pharmacology access to insights from major conferences, emerging research, and expert commentary Whether you’re a pharmacologist GPCR scientists, translational pharmacologists, biotech drug discovery teams, and decision-makers who Edition here ➤    Access all the news and upcoming events Hashtags: #GPCR #DrGPCR #BindingAffinity #Pharmacology

Pharmacology & Therapeutics   2016 , 165 , 164–177. https://doi.org/10.1016/j.pharmthera.2016.06.007 European Journal of Pharmacology   2017 , 799 , 58–66. https://doi.org/10.1016/j.ejphar.2017.01.040 . European Journal of Pharmacology   2018 , 839 , 40–46. https://doi.org/10.1016/j.ejphar.2018.09.008 . Trends in Pharmacological Sciences   2018 , 39  (2), 187–199. https://doi.org/10.1016/j.tips.2017.10.004 Biochemical Pharmacology   1973 , 22 (23), 3099–3108. https://doi.org/10.1016/0006-2952(73)90196-2 .

Because when true pharmacological profiling is essential—like detecting partial or inverse agonism—calcium If you're starting out in pharmacology, this lesson gives you the interpretive tools to ask smarter questions calcium assays with strategic clarity. 📍 Foundational Level | Calcium Assays 📚 Part of Terry Kenakin’s Pharmacology

GPCR Enthusiasts , Get ready for an exciting learning experience with our newly updated Principles of Pharmacology New Course Dates: Principles of Pharmacology I :  October 3, 10, 17, 24 (four sessions) Principles of Pharmacology II :  October 31, November 7, 14, 21, December 5 (five sessions) Courses Highlights Act Fast: Don’t miss this incredible opportunity to immerse yourself in the  Principles of Pharmacology and ' Advanced Data Analysis for GPCR Pharmacology' ."

Hello Dr.GPCR readers! This is Lucía from the Celtarys Research chemistry team.  For our very first post in this ecosystem, we wanted to highlight a huge part of our work at Celtarys Research: conjugation strategies. You can check what we do here on our website!   Conjugation strategies for small molecules are very versatile! In this case, we would like to focus on the synthesis of fluorescent probes. Traditionally, the most reliable and commonly used method is the amide coupling  using acid and amine .[ 1 ] This method has several advantages: it is usually very robust, good yields, reagents are found in most chem labs (like HATU, HoBT, EDCI etc.). Still, there are some downsides, such as the byproduct obtained by the O-acylisourea rearranging intramolecularly into the N-acylurea.[ 2]     NHS ester amide coupling  is the most suited for bioconjugation with proteins, DNA, etc, thanks to its reaction with the free amino groups present in these biomolecules. NHS esters are not very stable even in aqueous environment but they only need a slightly basic medium for the reaction to work, so they have to be used quickly and stored correctly. Not only do they work in aqueous medium, but also in aprotic solvents like DMF, where you will need to add a base such as TEA. [ 3]     Maleimide  conjugation with thiols  present Cys residues. This conjugation is very useful for tagging biomolecules and can also be used to develop fluorescent probes with small molecules. Its biggest advantage is the presence of Cys residues in proteins, although sometimes S-S bridge reduction is needed, and how quickly the reaction takes place. The biggest detractor? It’s reversible under non-reducing conditions. [ 4]     Other strategies include click chemistry,  more specifically, the CuAAC (Cu(I)- catalyzed azide-alkyne 1,3-dipolar cycloaddition), which is a very robust conjugation strategy to obtain linkers with a rigid moiety (the triazol). But it also presents some issues, such as synthesizing the as the presence of the copper catalyst, which has to be removed completely, otherwise it can quelate biomolecules or induce cell toxicity. [ 5]     At Celtarys’ we have our conjugation strategy - our own proprietary technology- which bypasses some of the issues seen before. There’s no need for any catalysts; all reagents will be incorporated in the structure of the final compound. The reaction is convergent, efficient and robust. Thanks to the unique linker structure we obtain, which can be divided into three differentiated parts, we can modify the rigidity of the linker as well as the physicochemical properties of the whole probe. This property comes from the wide chemical space this reaction can access – we can substitute one reagent and make an unprecedented combination, also using commercially available precursor, which improves the performance of the probes.  It also poses some disadvantages – just like acid-amine amide coupling, some byproducts are obtained during the synthesis. However, these are usually easily removable. Besides, it’s an eco-friendlier method, which always helps future-proof our probes!  References   (1) Brown, D. G.; Boström, J. Analysis of Past and Present Synthetic Methodologies on Medicinal Chemistry: Where Have All the New Reactions Gone?: Miniperspective. J. Med. Chem.   2016 , 59  (10), 4443–4458. https://doi.org/10.1021/acs.jmedchem.5b01409 .   (2) Sam, S.; Touahir, L.; Salvador Andresa, J.; Allongue, P.; Chazalviel, J.-N.; Gouget-Laemmel, A. C.; Henry De Villeneuve, C.; Moraillon, A.; Ozanam, F.; Gabouze, N.; Djebbar, S. Semiquantitative Study of the EDC/NHS Activation of Acid Terminal Groups at Modified Porous Silicon Surfaces. Langmuir   2010 , 26  (2), 809–814. https://doi.org/10.1021/la902220a .   (3) Fan, J.; Toth, I.; Stephenson, R. J. Chapter Three - Bioconjugated Materials in the Development of Subunit Vaccines. In Comprehensive Analytical Chemistry ; Verma, S. K., Das, A. K., Eds.; Elsevier, 2023; Vol. 103, pp 59–103. https://doi.org/10.1016/bs.coac.2023.02.005 .   (4) Fontaine, S. D.; Reid, R.; Robinson, L.; Ashley, G. W.; Santi, D. V. Long-Term Stabilization of Maleimide–Thiol Conjugates. Bioconjugate Chem.   2015 , 26  (1), 145–152. https://doi.org/10.1021/bc5005262 .   (5) Meldal, M.; Tornøe, C. W. Cu-Catalyzed Azide−Alkyne Cycloaddition. Chem. Rev.   2008 , 108  (8), 2952–3015. https://doi.org/10.1021/cr0783479 .

Rather than treating opioid pharmacology as a purely theoretical exercise, she collaborates with harm-reduction This approach makes her models not just rigorous, but translational—bridging the gap between receptor pharmacology That personal loss transforms complex receptor pharmacology into something immediate and human. Real-world data should guide how we build preclinical models. And GPCR pharmacology isn’t just an academic pursuit—it’s essential to understanding and responding to

detailed structure‐activity relationship that identifies small changes to the ligands that invert their pharmacological

First responders describe revivals that don’t feel like revivals, as if the body is still trapped in a pharmacological Catherine’s work lays the foundation for designing better interventions, from preclinical models to clinical

Consulting Philosophy Every successful GPCR program is a blend of scientific excellence  and operational precision

exactly what Terry’s Corner delivers this week: high-impact insight into GPCR allostery, crafted for pharmacologists Exploit probe dependence to shape precision pharmacology.  Want to avoid off-target effects? If you work on GPCRs across translational pharmacology, drug development, or molecular pharmacology, GPCR scientists, translational pharmacologists, biotech drug discovery teams, and decision-makers who

Every R&D team is under the same pressure: deliver validated targets, clean pharmacology, and translatable Allosteric Interactions Still Matter Orthosteric and allosteric interactions have been in pharmacology learn why this distinction is not just theory, but a practical framework to design cleaner, smarter pharmacology Equip your team with this literacy now to design cleaner pharmacology and accelerate smarter, safer programs lectures  that sharpen the tools you actually use in discovery A growing on-demand library  of expert pharmacology

December 2021 Perkins’ Head of Molecular Endocrinology and Pharmacology, Professor Kevin Pfleger, was appointed President of the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists Coincidentally, on the same day, Prof Pfleger was announced as a Fellow of the British Pharmacological ASCEPT is the peak professional society devoted to advancing excellence in Clinical and Experimental Pharmacology Established in 1966, ASCEPT is affiliated with the International Union of Basic and Clinical Pharmacology

August 2022 Dopamine D 1 receptor-mediated β-arrestin signaling: Insight from pharmacology, biology, We now summarize important pharmacological, molecular, and cellular studies relevant to D1-mediated β-arrestin-related discuss the importance of understanding the translatability of cell and animal models to have more precise

It’s rigorous pharmacology, but deeply tied to urgent public health needs.

GPCR scientists, translational pharmacologists, biotech discovery teams, and decision-makers who need

This section outlines the logic required to match preclinical models to patient physiology and avoid β-receptor partial agonists, showing how heart rate set-points under different anesthetics can flip observed pharmacology Subscribe today and get direct access to decades of pharmacology experience that turn complex systems Why Terry’s Corner Most pharmacology training freezes at equilibrium snapshots.

August 2022 A NanoBRET-Based H 3 R Conformational Biosensor to Study Real-Time H 3 Receptor Pharmacology monitor the activation state of G protein-coupled receptors are a useful addition to the molecular pharmacology

Yet, any pharmacologist who’s pushed beyond textbook theory knows: biology rarely plays fair. Schild analysis turns receptor pharmacology into detective work, spotlighting mechanistic fingerprints Modern pharmacology has powerful modeling software, yet Schild analysis remains the litmus test for mechanism Watch the course trailer 👇 Why Terry’s Corner Weekly pharmacology lectures by Dr. Built for pharmacologists refining tools, discovery teams solving bottlenecks, and leaders seeking credible

Corner , our founder Yamina Berchiche works closely with organizations to help them navigate receptor pharmacology Push the boundaries  of receptor pharmacology and its real-world applications.   📚 Terry’s Corner — The Only On-Demand Pharmacology Hub with Dr. GPCR  community, you already know about Terry’s Corner  — our exclusive, on-demand pharmacology series where Terry Kenakin breaks down receptor pharmacology, functional selectivity, and ligand bias in a

Yet some assumptions still shaping pharmacology workflows haven’t evolved as fast as today’s science. Unlock “Rethinking Affinity” Now Only in Terry's Corner _____ #GPCR #BindingAffinity #Pharmacology

Every step felt like it could make or break the result, The pace and precision of GPCR research today Today, success depends less on manual precision and more on experimental design, data interpretation, What started as hand-built assays on ice has become integrated platforms for drug discovery, systems pharmacology

Rethinking Affinity, A Critical Edge for Drug Hunters One of the most persistent misconceptions in pharmacology apparent affinity differences delays key milestones. 🗣️ “Thank you for bringing this (Principles of Pharmacology At Alkermes, Sokhom Pin built an in vitro pharmacology group from scratch—not just a lab, but a culture Weekly News : jobs, events, papers, industry updates Exclusive discounts on Terry’s Corner  digital pharmacology Access this week’s full Premium Edition here ➤ Hashtags: #GPCR #DrGPCR #BindingAffinity #Pharmacology

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

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

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

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

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

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

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

Early Access and Updates    Terry’s Corner is launching soon with monthly courses, AMAs, and real-world pharmacology