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transduction at GPCRs: Allosteric activation of the ERK MAPK by β-arrestin GPCR Binders, Drugs, and more Pharmacologically Proof-of-Concept Studies Sosei Heptares’ President & CEO Chris Cargill Wins Executive of the Year at the Citeline Pharma Chemotactic Cytokines GPCR Jobs Head of Human Resource Business Partners Senior Scientist, In vitro pharmacology - Crinetics Pharmaceuticals Senior Director, In vitro pharmacology - Crinetics Pharmaceuticals In vivo Antibody Discovery Research Scientist In Vitro Biologist/Molecular Pharmacologist Senior Vice President

Andrew Tobin for an incredible week filled with prestigious events, including receiving the British Pharmacological and TPD Structural Biology Platforms GPCR Events, Meetings, and Webinars December 10 - 12, 2024 | Pharmacology to GPCR Drug Discovery March 12 - 14, 2025 | NextGen Biomed 2025 March 25 - 28, 2025 | 10th German Pharm-Tox GPCR Jobs GPCR Molecular Pharmacologist Scientist - Biology Scientist I Cell Biology - Tectonic Therapeutic Research Associate - Professor Graeme Milligan Postdoc in Molecular Pharmacology - The Hauser Group

Terry Kenakin's "Applying Pharmacology to Drug Discovery" course at Dr. to advance novel anti-CCR8 antibody  for cancer immunotherapy Novo Holdings Portfolio Company Amolyt Pharma , 2024 | 11th Adhesion GPCR Workshop July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology Research Unit Postdoctoral Scholar – Synaptic physiology, optical imaging, substance use disorder, pharmacology Research Fellow Postdoctoral Fellow – Molecular Pharmacology of Feeding Behavior Director of Laboratory

Webinar - Antiverse: Engineering the Future of Drug Discovery (March 30, 2023) NEW Molecular Dynamics in Pharma (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 IRN I-GPCRNet (October 25 - 27, 2023) GPCR Jobs NEW Team Lead protein production and profiling NEW Pharmacologist

Tablet PK Study for its Oral Non-Peptide Small Molecule GLP-1 Receptor Agonist GSBR-1290 Crinetics Pharmaceuticals Treatment Of Congenital Adrenal Hyperplasia (CAH) And Acth-Dependent Cushing’s Syndrome (ADCS) Nxera Pharma to Receive $4.6 Million in Milestone Payments from Centessa Pharmaceuticals CB1 receptor inverse agonist , 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

Thrilling beginning to Principles of Pharmacology I We are excited to announce the start of our Principles of Pharmacology I course! Don’t miss this opportunity to advance your knowledge and skills in pharmacology! Modules: October 31st : The Eyes to See- The Importance of Pharmacologic Assays. Multi-Target Collaboration with Novartis to Discover and Develop Protein Therapeutics with Generative AI Nxera Pharma

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 .

Samuel Hoare on Advanced data analysis for GPCR pharmacology, which will be held on Thursdays between , Mark Schmeizl, had a great conversation about this position with Beth Fleck, Director of In Vitro Pharmacology at Crinetics Pharmaceuticals! MacDonald as Chief Executive Officer Nxera Pharma Announces Exclusive Supply and Distribution Agreement 2026 GPCR Jobs NEW Postdoc Position Principal Scientist, In vitro pharmacology Senior Associate Scientist

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.

Every Thursday at 10 AM EST: Principles of Pharmacology I October 3, 10, 17, 24 (four sessions) Topics : Pharmacologic activity measurement, mechanisms of action, and GPCR discovery strategies. Principles of Pharmacology II October 31, November 7, 14, 21, December 5 (five sessions) (we skipped The Principles of Pharmacology I & II BUNDLE is your key to mastering the field. platform; Carterra Ultra™ ushers in a new frontier in fragment and small molecule drug discovery Is the pharma

Gunnar Schulte, Lukas Grätz, Pawel Kozielewicz, et al. for their study on Frizzleds act as dynamic pharmacological Samuel Hoare on Advanced data analysis for GPCR pharmacology, which will be held on Thursdays between and Pharmacology Addex Therapeutics to Release Full-Year 2023 Financial Results and Host Conference Call on April 18, 2024 Nxera Pharma Notes Successful Development Progress of Partnered Schizophrenia 2026 GPCR Jobs NEW Principal Scientist, In vitro pharmacology Senior Associate Scientist - Global Research

Terry Kenakin's "Applying Pharmacology to Drug Discovery" course at Dr. pathways and two distinct high-affinity sites for succinate in succinate receptor 1/GPR91 Specific pharmacological development GPCR Events, Meetings, and Webinars March 13 - 15 | Biologics 2024 March 13 - 15 | 9th German Pharm-Tox , 2024 | 11th Adhesion GPCR Workshop July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology Research Fellow Postdoctoral Fellow – Molecular Pharmacology of Feeding Behavior Director of Laboratory

Samuel Hoare on Advanced data analysis for GPCR pharmacology, which will be held on Thursdays between Terry Kenakin’s Applying Pharmacology to Drug Discovery course. Continue to increase your knowledge of Pharmacology by joining this practical approach class today. Industry News Monash University pharmaceutical scientists honoured in NHMRC Research Excellence Awards Re-election of its Board and Executive Management Team and the Approval of Change of Company Name to Nxera Pharma

University We successfully started our Dr.GPCR University workshop, 'Advanced Data Analysis for GPCR Pharmacology Initiation of Phase 1 Clinical Study Evaluating Effects of NBI-1117567 in Healthy Adults Crinetics Pharmaceuticals Reports First Quarter 2024 Financial Results and Provides Business Update Nxera Pharma Operational Highlights and Consolidated Results for the First Quarter 2024 Crinetics Pharmaceuticals To Present Advancements 2026 GPCR Jobs Post Doctoral Fellow Postdoc Position Principal Scientist, In vitro Pharmacology Senior

GPCR University Course, ‘Applying Pharmacology to Drug Discovery,’ led by Dr. Research GPCR Events, Meetings, and Webinars March 13 - 15 | Biologics 2024 March 13 - 15 | 9th German Pharm-Tox , 2024 | 11th Adhesion GPCR Workshop July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology Research Unit Postdoctoral Scholar – Synaptic physiology, optical imaging, substance use disorder, pharmacology Research Fellow Postdoctoral Fellow – Molecular Pharmacology of Feeding Behavior Director of Laboratory

GPCR University Last week marked the beginning of our first Dr.GPCR University course, 'Applying Pharmacology coupled receptor-mediated vasocontraction in rat coronary arteries GPCRs involved in metabolic diseases: pharmacotherapeutic Board of Directors GPCR Events, Meetings, and Webinars February 20, 2024 | Career Opportunities in Pharmacology and Drug Discovery March 13 - 15 | 9th German Pharm-Tox Summit March 23 - 24, 2024 | Ligand Recognition , 2024 | 11th Adhesion GPCR Workshop July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology

Celebrating Excellence:   Patrick Sexton  and Arthur Christopoulos  Named Among Top 1% of Scientists in Pharmacology Pfleger ,  Peter J McCormick , Cristina Salmerón ,   Paul A Insel PGxDB: an interactive web-platform for pharmacogenomics novo antibodies look more like drugs  GPCR Events, Meetings, and Webinars December 10 - 12, 2024 | Pharmacology to GPCR Drug Discovery March 12 - 14, 2025 | NextGen Biomed 2025 March 25 - 28, 2025 | 10th German Pharm-Tox Research Associate - Professor Graeme Milligan Postdoc in Molecular Pharmacology - The Hauser Group

Pharmacological characterization of novel small molecule agonists and antagonists for the orphan receptor Multiple Myeloma Behind Friday's $161M IPO: A star scientist, GPCR drug discovery and a plan to challenge pharma (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. PhD student at Department of Drug Design and Pharmacology Software / database development postdoc at

with Domain Therapeutics and Université de Montréal for GPCR-Targeted Drug Discovery "Apr.19.2022 Ono Pharmaceutical

17th, 2024 Industry News Centessa Launches Phase 2 Trial of ORX750 for Narcolepsy and IH Crinetics Pharmaceuticals to GPCR Drug Discovery March 12 - 14, 2025 | NextGen Biomed 2025 March 25 - 28, 2025 | 10th German Pharm-Tox | BIO International Convention 2025 July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology Principal Scientist, Medicinal Chemistry PhD fellowship in GPCR mechanosensing Senior Scientist, GPCR Pharmacology Research Associate - Professor Graeme Milligan Postdoc in Molecular Pharmacology - The Hauser Group

GPCR University course, 'Applying Pharmacology to Drug Discovery,' led by Dr. and more Nanobody-Mediated Dualsteric Engagement of the Angiotensin Receptor Broadens Biased Ligand Pharmacology Pharmacological characterization and radiolabeling of VUF15485, a high-affinity small-molecule agonist and Drug Discovery March 13 - 15 | 9th German Pharm-Tox Summit March 23 - 24, 2024 | Ligand Recognition 2026 GPCR Jobs NEW Research Fellow NEW  Postdoctoral Fellow – Molecular Pharmacology of Feeding Behavior

GPCR University We're thrilled to share that all spots for the Applying Pharmacology to Drug Discovery Exhibition February 11 - 14, 2024 | 2024 BPS Annual Meeting NEW February 20, 2024 | Career Opportunities in Pharmacology and Drug Discovery March 13 - 15 | 9th German Pharm-Tox Summit March 23 - 24, 2024 | Ligand Recognition , 2024 | 11th Adhesion GPCR Workshop July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology

GPCR University course, Applying Pharmacology to Drug Discovery, led by Dr. The course covers basic pharmacology in four weekly segments and is open to all with a free site membership Conference and Exhibition February 11 - 14, 2024 | 2024 BPS Annual Meeting NEW March 13 - 15 | 9th German Pharm-Tox , 2024 | 11th Adhesion GPCR Workshop July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology

July 2022 "Not even a PIPE financing could save X4 Pharmaceuticals from enacting layoffs and trimming

June 2022 "CRN04894 Selected for Oral Presentation SAN DIEGO, June 8, 2022 — Crinetics Pharmaceuticals

GPCR University This week marks the beginning of our first Dr.GPCR University course, 'Applying Pharmacology Webinars February 11 - 14, 2024 | 2024 BPS Annual Meeting February 20, 2024 | Career Opportunities in Pharmacology and Drug Discovery March 13 - 15 | 9th German Pharm-Tox Summit March 23 - 24, 2024 | Ligand Recognition , 2024 | 11th Adhesion GPCR Workshop July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology

Trevena Announces Submission of New Drug Application in China for OLINVYK® by its Partner Jiangsu Nhwa Pharmaceutical The NDA was submitted by Trevena’s partner, Jiangsu Nhwa Pharmaceutical, and follows completion by Nhwa

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

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

Using a similar pharmacophore  to the one present in the A 2A AR probe CELT-300 , new fluorescent ligands Using a similar pharmacophore  to the one present in the A 2A AR probe CELT-300 , new fluorescent ligands Pharmacological Reviews   2025 , 77  (6), 100092. https://doi.org/10.1016/j.pharmr.2025.100092 . (2) British J Pharmacology 2022, 179 (14), 3496–3511. https://doi.org/10.1111/bph.15103 . (5) Borrmann, T Pharmacol. 2000, 362, 382-391. https://doi.org/10.1007/s002100000315 (7) Jacobson, K. A.