Search Results

Stay informed with the most recent developments in GPCR research and industry news. Brendan Creemer, Thomas Gardella, and Ross Cheloha for their work on Highly biased agonism for GPCR ligands GPCR Activation and Signaling Highly biased agonism for GPCR ligands via nanobody tethering Mechanistic deficits GPCRs in Cardiology, Endocrinology, and Taste The full-length TSH receptor is stabilized by TSH ligand orientation using a neurotensin receptor 1 peptide Illuminating the neuropeptide Y4 receptor and its ligand

2022 "As the only member of the CX3C chemokine receptor subfamily, CX3CR1 binds to its sole endogenous ligand However, the drug development of CX3CR1 is hampered partially by the lack of structural information. Here, we present two cryo-electron microscopy structures of CX3CR1-Gi1 complexes in ligand-free and CX3CL1

These structures reveal an agonist binding site for the oxysterol and a potential ligand entrance site Together, these findings provide new insight into how EBI2 is activated by an oxysterol ligand and will facilitate the development of therapeutic approaches that target EBI2-linked diseases."

protein-coupled receptors are a useful addition to the molecular pharmacology assay toolbox to characterize ligand agonism and inverse agonism on living cells in a microplate reader assay format upon stimulation with H3R ligands have further characterized this H3R biosensor on intact cells by monitoring the effect of consecutive ligand injections in time and evaluating its compatibility with photopharmacological ligands that contain a ready-to-use, high-throughput alternative for radioligand binding assays that in addition can also detect ligand

Once a ligand crosses into this intracellular space, it behaves differently, often much more favorably Same Affinity, Different Outcomes: Why Residence Time Matters More Two ligands. And while orthosteric ligands may never reach them, properly designed intracellular drugs can.

A small molecule ligand for the novel pain target, GPR171, produces minimal reward in mice. Monitoring the Reversibility of GPCR Signaling by Combining Photochromic Ligands with Label-free Impedance , Endocrinology, and Taste Structure-based design of novel melanin-concentrating hormone receptor-1 ligands New paradigms in purinergic receptor ligand discovery. Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential.

Hello GPCR friends👋, Stay informed with the latest developments in GPCR research and industry news! Ligand-dependent intracellular trafficking of the G protein-coupled P2Y6 receptor. NMR applications to GPCR recognition by peptide ligands. Application of computational methods for class A GPCR Ligand discovery. New paradigms in purinergic receptor ligand discovery.

Activation: GAIN Domain Unfolding and Dissociation in Adhesion GPCRs Molecular sensing of mechano- and ligand-dependent receptor GPR81 drives breast cancer growth and invasiveness through regulation of ECM properties and Notch ligand Genentech and NVIDIA Enter Into Strategic AI Research Collaboration to Accelerate Drug Discovery and Development Annual Meeting March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Summit March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating

conformational ensemble of CX3C chemokine receptor 1 (CX3CR1) and its interactions with antagonist and agonist ligands receptor 1 (CX3CR1), a member of the class A of G Protein-Coupled Receptors (GPCR) superfamily, and its ligand characterize the conformational ensemble of the receptor in the presence of its antagonist and agonist ligands the receptor conformational changes and described interactions within its key regions and the bounded ligands

G-protein-coupled receptors (aGPCRs)-a major family of GPCRs-play critical roles in the regulation of tissue development analyses indicated that the palmitoylation of Go can allosterically stabilize the critical residues in the ligand-binding pocket of GPR97 and increase the affinity of the ligand for GPR97.

to Win: The IP One Gamble After the success of their cAMP assay, Trinquet’s team took a risky bet: develop And this ethos continues: every product is just the beginning of a feedback loop, where customer data

Adhesion GPCRs The adhesion G-protein-coupled receptor mayo/CG11318 controls midgut development in Drosophila Structure, ligands, and roles of GPR126/ADGRG6 in the development and diseases GPCR Activation and Signaling electrostatic interactions Industry News Domain Therapeutics strengthens leadership team to spearhead global development Annual Meeting March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Summit March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating

November 2022 "Some G protein-coupled receptor (GPCR) ligands act as "biased agonists" that preferentially differential subcellular signaling contributes to the biased signaling generated by three endogenous ligands The signaling profile of CXCR3 changes as it traffics from the plasma membrane to endosomes in a ligand-specific

De Graaf for their excellent work on Comparative Study of Allosteric GPCR Binding Sites and Their Ligandability Molecular Insights into GPCR Function Comparative Study of Allosteric GPCR Binding Sites and Their Ligandability

Tackling the GPCR Imprecision Problem: Strategic Planning for Sustainable Progress in Complex Systems. In the high-stakes world of GPCR drug discovery , breakthrough science isn't enough. You can have the most brilliant minds and cutting-edge assays, but if your science isn't continuously integrated with your GPCR operational strategy and investment goals, even the most promising program can falter. This fundamental disconnect between the lab and the boardroom  is precisely where programs get stuck—not because of bad science, but because companies find themselves throwing more money and people at problems that could be solved with better systems. This reactive approach, driven by a "go fast" mindset, burns through precious capital and time, leaving both scientific teams and investors frustrated. Companies find themselves throwing more money and people at problems that could be solved with better systems . This reactive approach, driven by the prevailing wisdom of "going fast" and focusing only on the science, burns through precious capital and time, leaving both scientific teams and investors frustrated. This belief that we don't have time to build better systems is a costly miscalculation. It reminds me of a conversation I recently overheard: my oldest child complaining about having to do 'everything at the same time ,' only for the youngest to wisely respond, 'No, you just need to do one thing at a time .' This simple truth applies profoundly to the "go fast" culture in biotech. We believe we don't have time to build better systems, but in reality, our most brilliant and expensive minds are stuck with low-impact tasks due to a lack of systems thinking . My perspective on this challenge is shaped not by a 40-year journey at the bench, but by an expertise in systems thinking  and operational discipline . My work isn't just  about the latest and best assay; it's about the framework that ensures the right assay data leads to the right decision. This is the critical piece that often gets lost in the "go fast" culture—the integration of science with strategy and flawless execution. I’ve lived this firsthand, not just in theory, but by building these systems from the ground up. I understand that embracing a systematic approach can feel daunting, especially with the pressure to move quickly. At Dr. GPCR, we recognized this core problem. Our Chief Brainstorm Officer, Attila Foris , is building a system so transparent that anyone joining the company can integrate seamlessly. Every time a problem arises, we trace it back to its root cause, implementing changes that prevent its recurrence. This iterative process of continuous, planned improvement ensures you're always addressing the next critical area. This is the essence of de-risking GPCR programs through operational excellence. This kind of continuous improvement doesn't happen organically; it demands intentional planning and a systematic approach, ensuring every step forward is strategic and sustainable. The Role of Systems Thinking in GPCR Drug Discovery Systems thinking is the intentional practice of seeing the entire GPCR program as a single, interconnected entity. It's the opposite of a reactive approach, where problems are solved in isolation. It’s the fundamental framework for building your Precision Blueprint , ensuring every scientific detail, operational process, and strategic decision aligns to create a seamless, predictable pathway to success. What You'll Learn in This Series Over the next five bi-weekly installments, " The GPCR Precision Blueprint " series will unpack how to bridge this critical gap. I'll show you how to transform your drug discovery process from a series of disconnected efforts into a seamless, predictable, and de-risked pathway. Part 1: The GPCR Imprecision Problem : I'll reveal why reliance on hiring more people over investing in robust systems thinking  is a multi-million dollar mistake. We'll look at how overlooked operational details, such as misaligned data from diverse GPCR assay types or communication gaps in cross-functional collaboration , lead to critical costs. Part 2: The Data Disconnect : Discover how fragmented, unmanaged GPCR data  cripples scientific progress and strategic decision-making. Learn how to build an integrated data pipeline  that transforms this chaos into a strategic asset. Part 3: The Financial Friction : Explore how a lack of precise alignment between GPCR scientific milestones  and financial realities creates significant risk. Learn to tie your program's progress directly to your funding runway, incorporating crucial early commercial and medical foresight. Part 4: The Investor Imperative : Understand what investors truly prioritize beyond just great science. Learn to translate your program’s internal operational precision into a compelling, de-risked narrative  that builds confidence and secures critical venture capital . Part 5: Your Precision Blueprint : I'll tie it all together, providing a concise, actionable guide for implementing this holistic approach within your own GPCR operational strategy , emphasizing that precision is a continuous, intentional journey towards predictable success. The GPCR Precision Blueprint is more than a concept. If you're ready to move beyond the articles and build these systems for your own GPCR program, let's connect. I work with biotechs, VCs, and CROs to implement the framework that ensures every step forward is strategic and sustainable, offering precision scientific and operational guidance  to accelerate discovery . 🚀 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

Ligands must first partition into the surrounding membrane and take lipid paths to these sites. Remarkably, a significant part of the bound ligands appears exposed to the membrane lipids. experimental structures do not usually account for the surrounding lipids, and their apparent contribution to ligand

metadynamics-enhanced conformational sampling are used here to determine the different interactions of these two ligands The endogenous peptide ligand endomorphin-1 (EM-1) underwent almost no significant conformational changes This finding reveals a dynamic mechanism for the response of MOR to different ligands and provides a basis for the discovery of new ligands for MOR at the atomic level."

De Graaf   for their excellent work on Comparative Study of Allosteric GPCR Binding Sites and Their Ligandability biotechs hacking the cell signaling pathway From Structure to Solution: How Structural Biology Informs the Development Board GLP-1s like Ozempic are among the most important drug breakthroughs ever Goldman-backed drug developer Molecular Insights into GPCR Function Comparative Study of Allosteric GPCR Binding Sites and Their Ligandability

by NMR spectroscopy with stable-isotope labeled receptors GPCR Binders, Drugs, and more Orthosteric ligand collaborates with Exscientia plc in deal worth up to $674M 2023 Half-Year Financial Results and Exciting Developments at Aelis Farma Ion Channel Drug Developer Maxion Therapeutics Appoints Eva-Lotta Allan as Chair of its Meeting February 3 - 7, 2024 | SLAS2024 International Conference and Exhibition March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating

acting as agonist at human β3 adrenoceptors and exerting BRL37344-like effects on mouse metabolism Development Industry News Sosei Heptares and Verily Nominate First G-protein-coupled receptor Target for Therapeutic Development DKK 25 million to development of databases supporting medical research ‘Define your own success’: Duke Meeting February 3 - 7, 2024 | SLAS2024 International Conference and Exhibition March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating

Heydenreich, Michel Bouvier, Brian Kobilka, M Madan Babu, and their team's work on Molecular determinants of ligand GPCRs) Associated with Lambda-Cyhalothrin Detoxification in Cydia pomonella Molecular determinants of ligand autophagy-mediated NLRP3 degradation Methods & Updates in GPCR Research Direct Binding Methods to Measure Receptor-Ligand Annual Meeting March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Summit March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating

reproduction of C. elegans Alexei Sirbu , Paolo Annibale , et al., for their study on Cell swelling enhances ligand-driven Exclusive Deal for Scientists Residing and Working in Developing Nations If you live and work  in a developing This technique for studying cell receptors could have sweeping implications for drug development DeepCure in Cardiology, Endocrinology, and Taste Role of G protein coupled receptors in acute kidney injury Ligand-Dependent of Neurological Disease s Activation of GPR55 alleviates neuropathic pain and chronic inflammation Developmental

in brain intercellular signaling Are there sex differences in oxytocin and vasopressin V1a receptors ligand Prediction of Large, Complex Protein Structures Newly discovered adhesion GPCR mayo controls midgut development that is now part of Bristol Myers Squibb GPCR Events, Meetings, and Webinars March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating

Before your GPCR ligand ever meets its receptor, it meets the enzymes that determine whether it survives Discovery Program So what does that mean for discovery scientists designing the next generation of GPCR ligands Even the most elegant GPCR ligand can fail if it never reaches its receptor. Direct input  on future sessions—so topics match the hurdles your team faces in discovery and development

by a chemerin-derived agonist Functional profiling of the G protein-coupled receptor C3aR1 reveals ligand-mediated biased agonism GPCR Binders, Drugs, and more Design and structural validation of peptide-drug conjugate ligands Annual Meeting March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Summit March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating

Adhesion GPCRs Collagen VI Is a Gi-Biased Ligand of the Adhesion GPCR GPR126/ADGRG6. The G protein-coupled receptor neuropeptide receptor-15 modulates larval development via the transforming GPCR Binders, Drugs, and more Adenosine A2A Receptor (A2AAR) Ligand Screening Using the 19F-NMR Probe Structural and Molecular Insights into GPCR Function Structural insights into ligand recognition and

The arrangement of the seven transmembrane helices creates a ligand-binding cavity on the extracellular Activation in Class A GPCRs Ligand binding in the orthosteric site leads to diverse activation mechanisms The agonist ligands (CCL5, CCL3, and [6P4]CCL5) bind to the 7TM cavity with their N-termini adopting promiscuity within subfamilies, functionally selective biased ligands, and constitutively active and of chemokine binding and receptor activation will pave the way for significant advancements in the development

High-throughput screening for receptor ligands was booming, and Sokhom was at the center of it.

GPCR Activation and Signaling Ligand-dependent intracellular trafficking of the G protein-coupled P2Y6 Neurotensin receptor 1-biased ligand attenuates neurotensin-mediated excitation of ventral tegmental Computational insights into ligand-induced G protein and β-arrestin signaling of the dopamine D1 receptor Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. Engineering NEW Scientist—Immuno-Oncology Convergent Research - Senior Scientist, Cell-Based Assay Development

eyJ1IjoiaHR0cHM6Ly9kb2kub3JnLzEwLjExMTEvYnBoLjcwMDcyIiwiciI6ImUyZGZlOTFjLTM5YzgtNDA5Yi04NTUyLWI5NjUwNGRlNzc4MyIsIm0iOiJtYWlsX2xwIiwiYyI6IjAwMDAwMDAwLTAwMDAtMDAwMC0wMDAwLTAwMDAwMDAwMDAwMCJ9 The B2D consortium revives biodiversity as a source for selective GPCR ligands