Her team at InterAx models receptor signaling pathways as systems of time-dependent equations, then runs in Graz, she spent six and a half years at Novo Nordisk in early drug discovery, focused on incretin receptors With a well-constructed computational model and a small set of kinetic assays, one compound on one receptor The next challenge is multi-receptor, multi-disease complexity. The computational tools that now describe single receptors will need to extend to how multiple receptors

Protein Folding to GPCRs – How Dmitry transitioned from biophysics and protein folding to cannabinoid receptor Interdisciplinary Research & Future Directions – Exploring combinatorial drug actions, receptor interactions Nottingham, where he provides leadership in structural and biophysical pharmacology of G protein coupled receptors and ETH Zürich in Switzerland, changing his attention to structural pharmacology of G protein-coupled receptors In 2017 Dmitry became a full professor at the Centre of Membrane Proteins and Receptors, COMPARE, a joined

structural and pharmacological bases for hormone-mediated activation of G proteins by G protein-coupled receptors These approaches were invaluable to resolve the crystal structure of the beta2-adrenergic receptor (beta2AR We continue to utilize these data to better understand the basis for receptor-G protein specificity and This is an important perspective in the pursuit of receptor subtype-specific ligands, a major aspect Again, our intention is to target specific receptor subtypes.

GPCRs, Receptors of Infinite Variety When asked about his favorite GPCR, Nicoli refused to pick. .” – Alessandro Nicoli He emphasized that olfactory receptors , while underexplored, present an incredible Modeling the Invisible: Olfactory Receptors Nicoli’s work centers on predicting ligand binding and receptor – Alessandro Nicoli He shared a detailed case study of working on a specific odorant receptor (R5VK1) His research focuses on a group of 400 transmembrane proteins known as olfactory receptors, which mediate

and the University of Michigan shaped his scientific curiosity, particularly around G protein-coupled receptors His research centers on the beta-2 adrenergic receptor and GPR65 , a proton-sensing receptor with promising therapeutic potential of GPR65, especially in the context of cancer immunotherapy, and how understanding receptor My research has looked at the trafficking and signaling of adrenergic and proton-sensing receptors, with

Five scientists audit what AI can and can't do for GPCR drug discovery — from orphan receptors and biased Random-forest classifiers trained on known peptide ligands can find new orphan-receptor pairings. Olfactory GPCRs — which account for a large fraction of the receptor class — have been systematically Selected Quotes "My computational team told me, 'this receptor is not using arrestin to internalize. G protein-coupled receptors (GPCRs) mediate a vast variety of critical biological processes and provide

registers: the practical mechanics of holding a GPCR signaling lab together remotely; the continuity of receptor pipeline before the shutdown, including a newly accepted BRET-based platform for beta-1 adrenergic receptor , and illustrates how GPCR scientists reason about pharmacology problems well outside their primary receptor , with the beta-1 adrenergic receptor as a worked example. The beta-1 adrenergic receptor paper — a BRET-based platform for capturing downstream signaling, built

Sokhom recalls how binding assays at BMS introduced him to the depth and complexity of receptor pharmacology There’s allosterism, receptor desensitization… it opened a whole new world.” PhD entirely in the industry setting—efficient, targeted, and rooted in real-world projects like CGRP receptor He blends classical receptor pharmacology with biosensor technology, always adapting to new tools and About Sokhom Pin Sokhom Pin is a receptor pharmacologist with over 20 years of drug discovery research

Marro describes a Gq coupled receptor program in which four lead series with sub nanomolar calcium potency The discussion extends to biased GLP1 receptor agonists that favor membrane retention and faster recycling gastrointestinal and cardiovascular metabolic disease, including the discovery of small molecule GLP1 receptor Emax as a driver of in vivo efficacy - Setting a high bar for what counts as true biased agonism - Receptor Keeping GLP1 receptors at the membrane can shape the therapeutic profile Building on work from Stephen

Summary Arthur's Career Journey and Allosteric Receptors Yamina and Arthur discussed Arthur's career journey and his contributions to the field of pharmacology, with a focus on allosteric receptors and They also discussed their own research on chemokine receptors and the importance of understanding the and GRKs, with Arthur recounting his initial collaboration with Patrick Sexton on RAMPs and amylin receptors They also delved into the different signaling of Class B receptors and the potential for modulation at

From early discoveries in cyclic AMP signaling to uncovering ultrasensitive receptor responses at femtomolar ligand concentrations, her work highlights why receptor localization and protein complex assembly matter Inside This Episode How ultrasensitive GPCR signaling emerges from pre-assembled receptor–effector complexes Why receptor localization and scaffolding dramatically shift functional readouts in disease models. The moment when femtomolar ligand concentrations uncovered unexpected receptor sensitivity.

Overexpressing a receptor produces a big, convenient signal, but it distorts the pharmacology and drifts Along the way they discuss the receptors that simply refuse to yield an assay, from adhesion GPCRs to GLP-1 resurgence that returned GPCRs to the front of drug discovery De-orphanizing GPCRs, including receptors A single receptor can trigger a large, amplified cyclic AMP response, which makes overexpression assays For years the field's spotlight drifted to checkpoints and T-cell receptors.

In parallel, his earlier work on orphan receptor deorphanization used co-evolution analysis and machine Together, these projects represent a rare attempt to connect the molecular detail of receptor pharmacology with the population-scale reality of how those receptors behave in living patients. genetic variants across human populations Co-evolution and machine learning as a framework for orphan receptor Orphan receptors can be systematically approached through evolutionary logic Rather than screening compound

Duke University (1994-1997), where he and his colleagues investigated the role of G protein-coupled receptor kinases and beta-arrestin in regulating G protein-coupled receptor endocytosis, trafficking, and signaling His research career has focused on the investigation of the regulation of G protein-coupled receptors Institutes of Health Research (CIHR) for his research investigating the role of metabotropic glutamate receptor

the development of approaches to quantify ligand bias and the identification of beta-arrestin-biased receptors The main focus of his lab’s research is on the mechanisms underlying biased agonism at chemokine receptors The chemokine system is relatively unique in having multiple receptors and multiple ligands that display His group and others have shown that many of these ligands act as biased agonists for the same receptor

Duke University (1994-1997), where he and his colleagues investigated the role of G protein-coupled receptor kinases and beta-arrestin in regulating G protein-coupled receptor endocytosis, trafficking, and signaling His research career has focused on the investigation of the regulation of G protein-coupled receptors Institutes of Health Research (CIHR) for his research investigating the role of metabotropic glutamate receptor

, study multiple targets and signaling pathways, investigate target species variations, deorphanize receptors , and more Comprehensive Coverage >1500 Human GPCRs products, including: 90% Target coverage Orphan receptors cell line backgrounds Multiple Mechanisms of Actions (MOA) cAMP accumulation β-Arrestin recruitment Receptor validated portfolio for obesity and diabetes GPCR targets, including GLP-1, GIP, GCG, MC4, PYY, AMY receptors Apelin (APJ/AGTRL1) View representative data: GLP-1R multi-MOA profiling Eurofins DiscoverX's GLP-1 receptor

student visa was in the work, during which time I thoroughly reviewed the literature on the melanocortin receptor first project where I demonstrated that MRAP2 regulates the signaling of multiple G protein-coupled receptors contributed to an In-vivo project that showed that MRAP2 regulates the growth hormone secretagogue receptor necessary modification leading to a structural change granting the arrestins access to the core of the receptor Cone was the first to clone the melanocortin receptors (the GPCRs that led to the discovery of MRAP2)

recently their role in cancer was treated as marginal — a few curiosities around mas and muscarinic receptors side project nobody believed in to a recognized driver class in oncology, and explains why chemokine receptors His training began at the University of Buenos Aires on alpha-2 adrenergic receptors, continued at the Aberrant expression — a receptor in the wrong place at the wrong time, paired with autocrine or paracrine Early focus-formation assays using muscarinic receptors and carbachol produced transforming efficiencies

York) in 1990 and 1992, working with Ravi Iyengar on regulation/desensitization of the liver glucagon receptor His initial project to identify and clone taste receptors was unsuccessful, but led to the identification For this, we have worked in three main areas: the regulation of G protein-coupled receptor signaling particularly by the G protein-coupled receptor kinase (GRK) – beta-arrestin system, the coordination

Following this tremendous experience, he was recruited to be the Principal Investigator of the Receptor To broaden his biomedical skill-set Stuart next accepted the position of Head of the Receptor Pharmacology Stuart’s current research, in the Receptor Biology Lab, focuses on the development of novel GPCR-based Stuart Maudsley on the web Maudsley Lab LinkedIn Google Scholar ResearchGate Maudsley Lab on Facebook Receptor

York) in 1990 and 1992, working with Ravi Iyengar on regulation/desensitization of the liver glucagon receptor His initial project to identify and clone taste receptors was unsuccessful, but led to the identification For this, we have worked in three main areas: the regulation of G protein-coupled receptor signaling particularly by the G protein-coupled receptor kinase (GRK) – beta-arrestin system, the coordination

Following this tremendous experience, he was recruited to be the Principal Investigator of the Receptor To broaden his biomedical skill-set Stuart next accepted the position of Head of the Receptor Pharmacology Stuart’s current research, in the Receptor Biology Lab, focuses on the development of novel GPCR-based Stuart Maudsley on the web Maudsley Lab LinkedIn Google Scholar ResearchGate Maudsley Lab on Facebook Receptor

York) in 1990 and 1992, working with Ravi Iyengar on regulation/desensitization of the liver glucagon receptor His initial project to identify and clone taste receptors was unsuccessful, but led to the identification For this, we have worked in three main areas: the regulation of G protein-coupled receptor signaling particularly by the G protein-coupled receptor kinase (GRK) – beta-arrestin system, the coordination

York) in 1990 and 1992, working with Ravi Iyengar on regulation/desensitization of the liver glucagon receptor His initial project to identify and clone taste receptors was unsuccessful, but led to the identification For this, we have worked in three main areas: the regulation of G protein-coupled receptor signaling particularly by the G protein-coupled receptor kinase (GRK) – beta-arrestin system, the coordination

degree in biochemistry from Leipzig University (Germany) being already fascinated by G protein-coupled receptors They also discussed the challenges of studying metabolites and their receptors, the relationship between Challenges in Studying Metabolites and Receptors Claudia and Yamina discussed the challenges of studying metabolites and their receptors, particularly in relation to fermented foods. They also explored the potential for better tools to understand and discover new metabolites or receptors

explore the development of powerful multiplex tools designed to map GPCR-RAMP interactions across the receptor That curiosity laid the foundation for a broader investigation into receptor activity-modifying proteins The lab’s early partnership with students like Emily Lorenzen catalyzed a transition from single-receptor From Many to One: De-Orphanization and Precision Focus “You can use this system to de-orphanize receptors Instead of focusing on a single receptor, students now gravitate toward platforms , biosensors , and

Jean-Philippe Pin Jean-Philippe Pin participated in the discovery of metabotropic glutamate receptors been studying the allosteric modulation and activation mechanism of this family of G protein-coupled receptors His studies led to new concepts in the GPCR field, such as the activation of cell surface receptors by

These extraordinary receptors, about which there was not much known other than that they are huge and with the vast unknown biochemical and pharmacological territory that would be helpful to study orphan receptors Her postdoctoral work leads her to investigate a whole family of orphan receptors: adhesion GPCRs. With the little knowledge on these receptors available, there were multiple questions to tackle.

and worked closely with Dr Birgitte Holst studying structural and mechanistic properties of ghrelin receptor associated with obesity and other metabolic diseases, including GPR10, Melanocortin 4, Serotonin 2C and TRH receptors cell-based in vitro technologies to study mechanistic properties of GPCRs and understanding the dynamics of receptor Jacek shared his fascination with the growth hormone secretion receptor and the melanocortin 4 receptor Yamina, in turn, talked about her work on melanocortin receptors and an upcoming collaboration with a