Search Results

It has been applied to different GPCR binding assays, such as CXCR4, opioid receptors, CCK1 and CCK2. Acta Pharmacol Sin   2019 , 40  (3), 324–335. https://doi.org/10.1038/s41401-018-0164-x . (8)         J Pharmacol Exp Ther   1996 , 278 (3), 989–999. (12)      Martín-Fontecha, M.; Angelina, A.; Rückert Pharmacological Evaluation of New Constituents of “Spice”: Synthetic Cannabinoids Based on Indole, Indazole 1,4-Dihydroquinoline-3-Carboxamide Derivatives as New CB2 Cannabinoid Receptors Agonists: Synthesis, Pharmacological

September 2022 Dynamics of tumor-associated macrophages in a quantitative systems pharmacology model of immunotherapy in triple-negative breast cancer "Quantitative systems pharmacology (QSP) modeling is

Hello GPCR Minds,   This week, you'll learn all about Terry’s Pharmacology Corner, your new learning space focused on GPCR pharmacology. GPCR Updates Learn Pharmacology That Drives Discovery  – From Dr. Terry Kenakin   Terry’s Corner is your space focused on GPCR pharmacology designed just for you.  

Breakthroughs this week:  Potentiation of GPCR signaling by ATP and sugar monophosphates; Pharmacology You’ll explore how catalytic control, allosteric shifts, and CYP450 behavior rewrite the rules of pharmacology Kenakin — October 30, 12 PM EST Bring your toughest pharmacology questions and join Dr. GPCR scientists, translational pharmacologists, biotech discovery teams, and decision-makers who need

How do competing ligands slow or alter binding rates, and what does this tell you about real-world pharmacology candidates faster Unlock “Drug Binding Kinetics” Now Only in Terry’s Corner   ______ #DrugDiscovery #Pharmacology

This interest has been driving efforts to understand their pharmacology since the 1980s. CELT-335 was successfully used in assays to determine the pharmacological properties of Δ9-tetrahydrocannabinol binding of naturally occurring Δ9-tetrahydrocannabinolderivatives to cannabinoid CB1 and CB2 receptors, Pharmacological Zagzoog A et al ., In vitro and in vivo pharmacological activity of minor cannabinoids isolated from Tetrahydrocannabinolic acid alleviates collagen-induced arthritis: Role of PPARγ and CB1 receptors, British Journal of Pharmacology

optimization ensure access to the binding site with minimal unspecific interactions, while also tuning the pharmacological Br J Pharmacol. 2020 Mar;177(5):978-991. doi: 10.1111/bph.14953. Probing the pharmacology of G protein-coupled receptors with fluorescent ligands.

ACCESS data for Structure Therapeutics’ oral GLP-1 agonist aleniglipron, Principal Scientist—In Vitro Pharmacology More new courses arrive weekly in 2026, expanding coverage across GPCR pharmacology fundamentals. demand for clearer interpretation, stronger experimental design, and better decision-making across GPCR pharmacology

October 2022 Pharmacological targeting of cGAS/STING-YAP axis suppresses pathological angiogenesis and Pharmacological targeting of cGAS/STING-YAP signaling by both a small-molecule STING agonist, SR-717, Further, pharmacological targeting of cGAS/STING-YAP axis exhibits the potential to alleviate liver and

We’ve made some updates to the Principles of Pharmacology I & II courses, and we can’t wait for you Here’s the refreshed schedule: Principles of Pharmacology I October 3, 10, 17, 24 Principles of Pharmacology Don’t miss out on insightful resources like '   Applying Pharmacology to Drug Discovery ' and ' Advanced Data Analysis for GPCR Pharmacology .' Don’t miss your chance to dive into the Principles of Pharmacology I & II BUNDLE .

For decades, GPCRs have been the cornerstone of pharmacology. Projects in his group often begin with either: A new GPCR structure  ripe for exploration, or A pharmacological Carlsson’s group integrates modeling with mechanistic pharmacology. improved GPCR structures, and scalable experimental assays is shrinking the gap between modeling and pharmacology Forward The Carlsson lab exemplifies how c omputational biochemistry can meaningfully impact real-world pharmacology

April 2022 Applying Allosteric Modulator Pharmacology to Treat Dyskinesia and Other Movement Disorders Addex Therapeutics "Tim Dyer is the Co-Founder and CEO of Addex Therapeutics, which is focusing on the pharmacology

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 .

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

Is Your GPCR Program Slowing Down—Even With Good Data? You’re not alone. Most teams don’t stall because the science is weak. They stall because the data becomes a mess. I call it the Lego Bucket Problem : You’ve got CRO output, internal assay data, maybe even some promising signals. But there’s no blueprint. No structure. No clear path to your next milestone. Meetings drag. Decisions stall. And momentum quietly dies. The Hidden Cost of Good Science Without Systems I’ve seen this pattern again and again—across academia, biotech, and through close work with dozens of teams inside the Dr. GPCR Ecosystem. Strong science. Promising data. But no systems to turn it into momentum. Data arrives too fast and too fragmented CROs deliver output without clear integration Teams chase the wrong assays, too late to pivot Milestones slip—and nobody realizes until it’s too late Failing fast? Not possible when nothing’s built to surface the right  insights early. That’s Why I Built Yamina’s Consulting Corner This is not “advising.” This is embedded consulting for biotech and VC teams who need to move fast —without compromising scientific integrity. Unlike traditional advisors, I'm not just observing; I'm part of your team . This allows me to experience your challenges firsthand, identify roadblocks faster , and i mplement solutions from within , ensuring genuine buy-in and lasting momentum. Here’s what I bring: Biology-First Strategy I’ve designed GPCR assays, led collaborations across research environments, and translated complex data into action. I know how to ask the right scientific questions—and when to shift from analysis to execution. Systems That Drive Execution No more disconnected slides and 6-week meeting cycles. I install simple tools that surface insights, align your team, and keep momentum moving. True Embedded Partnership I review CRO scopes, flag risks early, and sit in on your strategic calls. I’m not watching from the sidelines—I’m driving with you. Real-Time Global Insight As founder of Dr. GPCR, I’m connected to 1,300+ scientists and decision-makers worldwide. That network gives me a constant pulse on what’s working—and what’s next. Who I Work With ✅ Biotech Teams  – Especially those lacking in-house GPCR leads or overwhelmed by CRO data chaos. ✅ Venture Capital Firms  – Looking to accelerate, troubleshoot, or validate GPCR assets in their portfolio. ✅ Contract Research Organizations (CROs)  – Wanting to better align with biotech clients and deliver real  insight, not just data. My Consulting Philosophy Every successful GPCR program is a blend of scientific excellence  and operational precision . One without the other will quietly kill your momentum. My work is rooted in: ✔️ Scientific Integrity ✔️ Operational Discipline ✔️ Collaborative Partnership Let’s Get Your GPCR Program Moving Again Whether you’re building from scratch or recovering from a stall, I’ll help you move faster—with fewer blind spots, tighter execution, and a clear line of sight to your next key decision. 🚀 Book your free 30-minute strategy call Let’s unlock the momentum your GPCR program needs. 👉 https://calendly.com/drgpcr/yamina-corner Or explore how we can work together: 👉 Yamina.org 🔑 Key Takeaways ✅ Even strong science stalls without operational structure ✅ Scattered data = missed insights = wasted time ✅ You can’t fail fas t if you can’t see the problems early ✅ Most teams don’t need more data— they need clarity ✅ Yamina’s Corner helps teams move from data chaos to decisive action ✅ This is hands-on support —not passive advising p.s: Still unsure if this is the right fit? Let’s talk through your program—no pitch, just clarity.

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

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

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

Early Access and Updates    Terry’s Corner is launching soon with monthly courses, AMAs, and real-world pharmacology A MOR-positive allosteric modulator (BMS-986122) selectively enhances opioid signaling  through specific

What started as hand-built assays on ice has become integrated platforms for drug discovery, systems pharmacology