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He is particularly excited by the novel application of PAMs in chronic and neuropathic pain models , including the neuroma model , which is typically opioid-insensitive. Discovering breakthrough results in neuroma pain models via a spontaneous collaboration. This project involves molecular pharmacology in cell models to determine binding sites and mechanisms of allostery, as well as efficacy studies in mouse and rat models of acute and chronic pain.

Can models predict drug outcomes? Jens Carlsson shares how GPCR modeling is moving from explanation to real prediction in drug discovery . << Back to podcast list Strategic Partner(s) Model. Jens Carlsson What if models didn’t just explain the past — but could truly predict what comes next? Yamina Berchiche to share his unconventional journey from aspiring engineer to GPCR modeler.

biased agonism, and incorporates computational and mathematical modelling, structural and chemical biology , molecular and cellular pharmacology, medicinal chemistry, and preclinical models of behaviour and disease The conversation ended with Arthur's ongoing research and his development of a new operational model. model for allosteric modulation, emphasizing the balance between mechanism and empiricism. importance of establishing the correct disease context, setting up appropriate assays, and understanding the models

realities of using fluorescence-based assays, the challenge of translating in vitro pharmacology to in vivo models How integrating antibody-based modalities has expanded options for hard-to-drug GPCR targets. Teams expanding into antibody or biologic modalities for challenging GPCR targets.

, and confronting the true-negatives problem that quietly breaks so many published models. True negatives quietly wreck biological models. Most published models rely on inferred negatives — genes or molecules assumed inactive by convenience , the model's predictions changed radically. 37:01 Reading GPCR signaling dynamics with computational models 39:53 Generative models, scoring functions

Each session explores mechanistic models, translational challenges, and real-world therapeutic implications These GPCR webinars focus on conceptual frameworks, models, and translational insight that apply across introduce key concepts, the overall level is advanced and assumes familiarity with pharmacological models Topics may include: Receptor efficacy and operational models Allosteric modulators (PAMs and NAMs) Biased They provide exposure to current thinking, advanced modeling approaches, and expert interpretation of

Before focusing on the development of innovative mathematical modeling and simulation methods for drug They explored the potential of merging mathematical models with biology, the complexities of GPCRs within Integrating Mathematical Models and Biology: A Fascinating Discussion Yamina and Aurelien Rizk had a conversation about the importance of merging mathematical models and biology. and relevance of mathematical models in systems biology and pharmacology.

Livingston on allosteric opioid modulators, receptor internalization, and navigating the transition from research to biotech. << Back to podcast list Strategic Partner(s) Kathryn Livingston: Allosteric Opioid Modulators The first allosteric modulators of opioid receptors were discovered through an academic-industry collaboration Equilibrium vs. dynamic frameworks for studying receptor biology The Field Application Scientist as a career model Allosteric opioid modulators bypass the orthosteric site entirely Rather than competing with morphine

At UCSF, he develops structural models of GPCRs using sparse experimental data - combining restraints His fluency in both bench and computational languages shapes how he builds models and how he interprets Rather than a setback, it became a forced pivot into computation at precisely the moment his modeling Bench experience as a modeling guardrail Knowing what an EC50 means experimentally, or what a Bmax implies Bender credits his time at the bench with preventing the kind of over-interpretation that models built

Crauwels emphasizes the critical role of well-annotated experimental data for training predictive models Her work integrates bioinformatics, protein modeling, and experimental collaboration to support GPCR can significantly improve computational models. “Garbage in, garbage out—computational models depend entirely on the quality of experimental data.” the models.

Alessandro Nicoli shares how he models olfactory GPCRs with AlphaFold, mentors students, and builds science “AlphaFold gave us a face to those proteins… now we have 400 models to start with.” – Alessandro Nicoli Build predictive models to discover new ligands . About Alessandro Nicoli Alessandro Nicoli is currently a PhD student in the Molecular Modeling group Stefano Moro, where he worked on integrated Nuclear magnetic resonance (NMR) and computational modeling

Antonella Di Pizio on building computational models for GPCRs with almost no crystal structures and almost TAARs look more classical than most chemosensory GPCRs — and that matters for modeling. Di Pizio's workflow is deliberately iterative: build the model, predict binding-site residues, send them out for mutagenesis, fold the experimental results back into the model, rebuild. Collaborators are not recipients of finished predictions — they are partners embedded in the modeling

Her team at InterAx models receptor signaling pathways as systems of time-dependent equations, then runs kinetic assays to refine the models and extract ten to fifteen pharmacological parameters from what Model first, pipette second. InterAx treats GPCR pharmacology the way engineers treat aircraft design: build the mathematical model signaling pathways first, then use controlled kinetic assays as the "wind tunnel" that refines the model

postdoctoral role at the Polytechnic University of Turin (Italy), where he developed coarse-grained models tenure-track position, his research spans the development of computational methods such as structure-based models

Alex Serafini shares why pain research must start with real-world behavior and models before drilling Research Playbook Looking ahead, Serafini’s vision is bold: build a lab that develops translational models He's equally focused on sex differences in pain processing and the failure of "one-size-fits-all" models Whether it’s challenging legacy targets, redefining preclinical models, or exploring the epigenetic inheritance He aspires to become a physician-scientist, with a focus on translational in vitro and in vivo model

and blood-brain barrier dysfunction in vertebrate models. completing her PhD in Germany and her postdoctoral work at Columbia University, where she worked on ALS models adhesion GPCR research in Drosophila - CRISPR, epitope tagging, and knockout strategies The logic of model ortholog has been associated with vascular malformations and blood-brain barrier dysfunction in vertebrate models That thread, from a behavioral assay in a fly larva to a clinical phenotype in mice, is what gives the model

strategies to express, reconstitute and assay engineered GPCRs using the visual pigment rhodopsin as a model that stemmed from this work, such as the concept of “functional micro-domains” and the “helix movement model Tom’s lab also pioneered the early use of computational homology modeling, molecular dynamics simulations

agonist depending on receptor tone Quantitative pharmacology as rescue operation — using operational models A quantitative model can turn an artifact into pharmacology. Early in her postdoc, Dr. The resolution came not from a new experiment but from a model — protean agonism, as Kenakin had just in Bouvier's lab 05:30 — The side project that became the real work 08:22 — Protean agonism and the model So that is why I got so into the models — in order to salvage my project."

Duvall emphasizes the value of model systems and cross-species discoveries in GPCR biology. How dissecting receptor function in non-neuronal tissues uncovers new parallels to human gut-brain communication If you often translate receptor mechanism findings from model organisms to human systems. If you want to expand high-throughput or fluorescence-based assay strategies to non-traditional models Pew Scholarship, she continues to drive efforts to decode how evolutionarily conserved GPCR pathways modulate

From her early doubts to designing preclinical models of fentanyl and xylazine overdose, she reflects The methods used to measure respiratory depression in live models. shut down breathing through different mechanisms—work that blends receptor pharmacology, preclinical models

the University of Illinois at Chicago has spent years pulling apart that asymmetry — combining mouse models Her research integrates behavioral pharmacology, ligand-directed signaling, and mouse models of migraine appear to relieve the same symptoms — pain, negative affect, and aura-related signs in preclinical models Her next career step took her to AstraZeneca as a postdoctoral trainee, where she studied animal models Andrew Charles that who specialized in animal models of migraine and delta-opioid receptors as a therapeutic

including structural biology and proteomics, molecular biology and biochemical enzymology, primary and model cell culture, and transgenic, knockout, knock-in and conditional models of mouse physiology and behavior

including structural biology and proteomics, molecular biology and biochemical enzymology, primary and model cell culture, and transgenic, knockout, knock-in and conditional models of mouse physiology and behavior

including structural biology and proteomics, molecular biology and biochemical enzymology, primary and model cell culture, and transgenic, knockout, knock-in and conditional models of mouse physiology and behavior

including structural biology and proteomics, molecular biology and biochemical enzymology, primary and model cell culture, and transgenic, knockout, knock-in and conditional models of mouse physiology and behavior

Tools That Changed GPCR Pharmacology G-protein-coupled receptors were once described through a simple model The model was clean, teachable, and wrong in ways that took decades to prove. SCIENTIFIC THEMES OF THE CONVERSATION The limits of the binary receptor model and what inverse agonism Every receptor his lab has studied was selected because it was the right model for a question that was The divide illustrated something Bouvier has observed repeatedly: mental models, once useful, can become

During these four sessions, you'll dive into: Advanced pharmacokinetic modeling The Druglike Quality ✅ Practical Quantification of Allosteric Modulation – May 1, 2025 ✅ Applying the Black/Leff Operational Model to Predict Agonism – October 2, 2025 Premium Members save 25% on enrollment. 2nd GPCR signaling and drug discovery Symposium & Workshop NEW April 2 - 3, 2025 | New therapeutic modalities

Cancer Research, 2014) and GPCRs (Feigin, et al., PNAS, 2014) in breast cancer pathogenesis, using mouse models Mike also spoke about his initial struggles during his Ph.D., such as a difficult model system and a age and his desire to gain more knowledge about cancer biology led him to transition into using mouse models asked about his move from in vitro to in vivo work, and Mike explained that he wanted to use better models Yamina proposed further exploration of dosage and length of treatment in a mouse model and suggested

Why receptor localization and scaffolding dramatically shift functional readouts in disease models. validation under real experimental constraints, Tried to map signaling heterogeneity in disease-relevant models

Real-world case studies and data-driven models for pipeline prioritization, resource allocation, and Find the right collaboration model for your program.