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A collaboration between chemistry and biology sparked a GPCR imaging breakthrough, leading to new chemical probes for GLP-1R visualization in real tissue. Home → Flash News → A GPCR imaging breakthrough that didn’t start in a grant proposal A GPCR imaging breakthrough that didn’t start in a grant proposal Published on December 3, 2025 Category It started with a cold email. A young chemist, Dr. Johannes Broichhagen, was asked if he could synthesize a molecule “when you’re back in Munich.” That small moment pulled him into islet biology, confocal imaging, and a collaboration that would reshape how GLP-1R is visualized in real tissue. The new blog takes you behind the scenes — the London trip, the early confocal experiments, the pivot to chemical probes, and the trust-driven partnership that sparked a new era in GPCR imaging. If you care about chemical biology, receptor visualization, or building tools that actually work in complex systems, this one is worth reading. 🔗 Read the full story : https://www.ecosystem.drgpcr.com/post/how-collaboration-sparked-a-gpcr-imaging-breakthrough-in-chemical-biology Previous Next Recent Articles Why Biotech Fundraising Fails Due to Intellectual Property Gaps 👉 Why has intellectual property become a first-order fundraising signal? Biotech fundraising has undergone a subtle yet significant shift. Capital still exists, but investors are making decisions earlier and filtering more carefully . As a result, intellectual property is no longer something that comes up late in the process. 👉 It has become an early signal of whether a biotech company is fundable at all. This shift does not mean founders need more patents or heavier legal Attila Foris 5 days ago The Hidden Operating Cadence That’s Actually Driving Your Biotech Founders love the idea that a new year, or a new quarter, will reset the company. But here’s the uncomfortable truth: 👉 Your biotech is already running on an operating cadence you didn’t consciously design. And that cadence is shaping everything: timelines, decisions, investor calls, BD traction, internal focus. Most CEOs think they’re steering the strategy. 👉 In reality, their operating cadence is steering them. And until you see it, you can’t change it. Operating cadence Attila Foris Dec 24, 2025 GPCR Binding Affinity Experiments: Interpreting Data With Confidence as We Head Into 2026 As scientists, we know curves don’t equal clarity. As 2025 comes to a close, this final edition of Weekly News focuses on how GPCR binding affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development timelines long before anyone notices. The goal isn’t more data. It’s cleaner interpretation. And that’s exactly what carries strong discovery programs into 2026. Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift You Don’t Feel Until It’s Too Late 👉 Every early-stage biotech reaches a moment where the science finally starts clicking… and the company quietly stops doing anything else. BD conversations stay warm but motionless. Investor updates become thinner. Internal meetings slowly morph into scientific colloquia instead of decision-making forums. 👉 The uncomfortable truth: your company is doing a lot of science and very little building. No drama. No blow-ups.Just Attila Foris Dec 17, 2025 Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand, measure signal, fit a curve. Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves nothing like the idealized systems we learned in textbooks. GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry and time. The result is a recurring pattern across programs—clean data that is not actually telling the truth. Orthosteric bi Terry's Desk Dec 16, 2025

Discover how Dr. Jens Carlsson’s lab at Uppsala University is redefining GPCR drug discovery with predictive molecular modeling that forecasts receptor behavior—before the first assay begins. Home → Flash News → ep 175 with jens carlsson clip 1 Can your model actually predict the outcome of a GPCR experiment? Published on October 27, 2025 Category Dr. GPCR Podcast “Explain” is no longer enough. Can your model actually predict the outcome of a GPCR experiment? At Uppsala University, Dr. Jens Carlsson and his team are redefining what computational modeling means in drug discovery. Their lab doesn’t just simulate receptor-ligand interactions after the fact; they aim to forecast receptor behavior before the first assay is run. By integrating molecular docking, molecular dynamics, and machine learning, they design ligands with the goal to anticipate biological outcomes. This kind of predictive modeling challenges the traditional role of computation in pharmacology, where models have too often served as post hoc rationalizations. But Carlsson’s lab stands out for another reason: knowing when not to predict. His team is candid about the limits of their models. If the resolution isn't good enough, or if the data is too uncertain, they’re not afraid to say, “We don’t know.” That scientific humility (combined with deep collaborations with medicinal chemists and pharmacologists) is exactly what makes their predictions so useful. This episode is essential listening for anyone thinking seriously about translational pharmacology and the future of GPCR drug discovery. 🎧 Explore how predictive modeling is reshaping GPCR science in this Dr. GPCR Podcast episode: model predict discover #DrGPCR #GPCR #MolecularModeling #PredictivePharmacology #DrugDiscovery Previous Next Recent Articles Why Biotech Fundraising Fails Due to Intellectual Property Gaps 👉 Why has intellectual property become a first-order fundraising signal? Biotech fundraising has undergone a subtle yet significant shift. Capital still exists, but investors are making decisions earlier and filtering more carefully . As a result, intellectual property is no longer something that comes up late in the process. 👉 It has become an early signal of whether a biotech company is fundable at all. This shift does not mean founders need more patents or heavier legal Attila Foris 5 days ago The Hidden Operating Cadence That’s Actually Driving Your Biotech Founders love the idea that a new year, or a new quarter, will reset the company. But here’s the uncomfortable truth: 👉 Your biotech is already running on an operating cadence you didn’t consciously design. And that cadence is shaping everything: timelines, decisions, investor calls, BD traction, internal focus. Most CEOs think they’re steering the strategy. 👉 In reality, their operating cadence is steering them. And until you see it, you can’t change it. Operating cadence Attila Foris Dec 24, 2025 GPCR Binding Affinity Experiments: Interpreting Data With Confidence as We Head Into 2026 As scientists, we know curves don’t equal clarity. As 2025 comes to a close, this final edition of Weekly News focuses on how GPCR binding affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development timelines long before anyone notices. The goal isn’t more data. It’s cleaner interpretation. And that’s exactly what carries strong discovery programs into 2026. Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift You Don’t Feel Until It’s Too Late 👉 Every early-stage biotech reaches a moment where the science finally starts clicking… and the company quietly stops doing anything else. BD conversations stay warm but motionless. Investor updates become thinner. Internal meetings slowly morph into scientific colloquia instead of decision-making forums. 👉 The uncomfortable truth: your company is doing a lot of science and very little building. No drama. No blow-ups.Just Attila Foris Dec 17, 2025 Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand, measure signal, fit a curve. Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves nothing like the idealized systems we learned in textbooks. GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry and time. The result is a recurring pattern across programs—clean data that is not actually telling the truth. Orthosteric bi Terry's Desk Dec 16, 2025

Home → Flash News → Unlock your pharmacology potential with Terry’s Corner. No fluff. Just clear, on-demand insight from Dr. Terry Kenakin—built for scientists at every level. 🟢 Building core expertise? Learn dose-response, agonism, binding, bias, kinetics, and the models that build real confidence. 🟢 Driving drug discovery? Apply pharmacology to selectivity, ADME, early safety, and smarter decision-making. 🟢 Already a drug hunter? Sharpen your edge with allosteric modulation, residence time, molecular dynamics, and translational PK/PD. Learn on-demand. Apply immediately. Early access begins July 1 → https://www.terrykenakin.com #pharmacology #GPCRscience #drugdiscovery #TerrysCorner #biotechtraining Published on June 28, 2025 Category Terry's Corner Unlock your pharmacology potential with Terry’s Corner. No fluff. Just clear, on-demand insight from Dr. Terry Kenakin—built for scientists at every level. 🟢 Building core expertise? Learn dose-response, agonism, binding, bias, kinetics, and the models that build real confidence. 🟢 Driving drug discovery? Apply pharmacology to selectivity, ADME, early safety, and smarter decision-making. 🟢 Already a drug hunter? Sharpen your edge with allosteric modulation, residence time, molecular dynamics, and translational PK/PD. Learn on-demand. Apply immediately. Early access begins July 1 → https://www.terrykenakin.com #pharmacology #GPCRscience #drugdiscovery #TerrysCorner #biotechtraining Previous Next Recent Articles

Home → Flash News → Forget one receptor at a time. Go big.Ep.167 of the Dr.GPCR Podcast with Tom Sakmar & Ilana Kotliar is about scaling GPCR research with multiplexing, miniaturization, and collaboration. The tools are built. The data is free. What will you ask next? 📲 Dive in: Ep 167 with Drs. Tom Sakmar & Ilana Kotliar #GPCRtraining #GPCRresearchcommunity #DrGPCR #GPCRdata Published on June 5, 2025 Category Dr. GPCR Podcast Forget one receptor at a time. Go big.Ep.167 of the Dr.GPCR Podcast with Tom Sakmar & Ilana Kotliar is about scaling GPCR research with multiplexing, miniaturization, and collaboration. The tools are built. The data is free. What will you ask next? 📲 Dive in: Ep 167 with Drs. Tom Sakmar & Ilana Kotliar #GPCRtraining #GPCRresearchcommunity #DrGPCR #GPCRdata Previous Next Recent Articles Why Biotech Fundraising Fails Due to Intellectual Property Gaps 👉 Why has intellectual property become a first-order fundraising signal? Biotech fundraising has undergone a subtle yet significant shift. Capital still exists, but investors are making decisions earlier and filtering more carefully . As a result, intellectual property is no longer something that comes up late in the process. 👉 It has become an early signal of whether a biotech company is fundable at all. This shift does not mean founders need more patents or heavier legal Attila Foris 5 days ago The Hidden Operating Cadence That’s Actually Driving Your Biotech Founders love the idea that a new year, or a new quarter, will reset the company. But here’s the uncomfortable truth: 👉 Your biotech is already running on an operating cadence you didn’t consciously design. And that cadence is shaping everything: timelines, decisions, investor calls, BD traction, internal focus. Most CEOs think they’re steering the strategy. 👉 In reality, their operating cadence is steering them. And until you see it, you can’t change it. Operating cadence Attila Foris Dec 24, 2025 GPCR Binding Affinity Experiments: Interpreting Data With Confidence as We Head Into 2026 As scientists, we know curves don’t equal clarity. As 2025 comes to a close, this final edition of Weekly News focuses on how GPCR binding affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development timelines long before anyone notices. The goal isn’t more data. It’s cleaner interpretation. And that’s exactly what carries strong discovery programs into 2026. Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift You Don’t Feel Until It’s Too Late 👉 Every early-stage biotech reaches a moment where the science finally starts clicking… and the company quietly stops doing anything else. BD conversations stay warm but motionless. Investor updates become thinner. Internal meetings slowly morph into scientific colloquia instead of decision-making forums. 👉 The uncomfortable truth: your company is doing a lot of science and very little building. No drama. No blow-ups.Just Attila Foris Dec 17, 2025 Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand, measure signal, fit a curve. Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves nothing like the idealized systems we learned in textbooks. GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry and time. The result is a recurring pattern across programs—clean data that is not actually telling the truth. Orthosteric bi Terry's Desk Dec 16, 2025

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Developing a PROTAC to Degrade the Constitutively Active Onco-GPCR in Uveal Melanoma Date & Time Friday, November 3rd / 4:20 PM About Victoria Rasmussen "Victoria Rasmussen is a graduate fellow in Dr. Thomas Sakmar’s laboratory at Rockefeller University, where she studies the signaling and degradation of G protein-coupled receptors. She completed her undergraduate education at Providence College, receiving a B.S. in Biology and a B.A. in Psychology. During her time at Providence College, she received the Walsh Grant Fellowship to develop novel methods of synthesizing 2-imidazoline scaffolds to be used as proteasome modulators in the laboratory of Travis Bethel. Victoria started her Ph.D. at the Tri-Institutional Ph.D. program in Chemical Biology, where she joined the lab of Thomas Sakmar at Rockefeller University. She is currently working to understand the signaling and degradation of GPCRs in disease states to help test the feasibility of using protein-targeted degradation as a therapeutic strategy. " Victoria Rasmussen on the web Tri-Institutional PhD Program Chemical Biology LinkedIn Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Discover how enzyme inhibition can enhance drug discovery strategies. Explore inhibition modes, CYP450 allostery, and insights from Dr. Eric Trinquet in this week's news. Home → Flash News → Weekly News October 16 Published on October 16, 2025 Category GPCR Weekly News Enzymes decide which molecules get a real shot at efficacy. This week’s Weekly News is your practical guide to building enzyme inhibition into discovery—not as a checkbox, but as a strategy. We unpack inhibition modes (competitive, noncompetitive, mixed, uncompetitive), the messy truth of CYP450 allostery and DDIs, and why allosteric control can protect potency in substrate-rich environments. Plus: a mindset masterclass from Dr. Eric Trinquet —how structured play turns into assays and why serendipity belongs in your build process. And a tertiary read on ciliary micro-domains linking OPN3/MCR signaling to appetite and skin biology. Read the full Weekly News ➤ https://lnkd.in/eWkAphen If this helped, pass it along to a colleague who needs the signal. #DrGPCR #GPCR Previous Next Recent Articles Why Biotech Fundraising Fails Due to Intellectual Property Gaps 👉 Why has intellectual property become a first-order fundraising signal? Biotech fundraising has undergone a subtle yet significant shift. Capital still exists, but investors are making decisions earlier and filtering more carefully . As a result, intellectual property is no longer something that comes up late in the process. 👉 It has become an early signal of whether a biotech company is fundable at all. This shift does not mean founders need more patents or heavier legal Attila Foris 5 days ago The Hidden Operating Cadence That’s Actually Driving Your Biotech Founders love the idea that a new year, or a new quarter, will reset the company. But here’s the uncomfortable truth: 👉 Your biotech is already running on an operating cadence you didn’t consciously design. And that cadence is shaping everything: timelines, decisions, investor calls, BD traction, internal focus. Most CEOs think they’re steering the strategy. 👉 In reality, their operating cadence is steering them. And until you see it, you can’t change it. Operating cadence Attila Foris Dec 24, 2025 GPCR Binding Affinity Experiments: Interpreting Data With Confidence as We Head Into 2026 As scientists, we know curves don’t equal clarity. As 2025 comes to a close, this final edition of Weekly News focuses on how GPCR binding affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development timelines long before anyone notices. The goal isn’t more data. It’s cleaner interpretation. And that’s exactly what carries strong discovery programs into 2026. Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift You Don’t Feel Until It’s Too Late 👉 Every early-stage biotech reaches a moment where the science finally starts clicking… and the company quietly stops doing anything else. BD conversations stay warm but motionless. Investor updates become thinner. Internal meetings slowly morph into scientific colloquia instead of decision-making forums. 👉 The uncomfortable truth: your company is doing a lot of science and very little building. No drama. No blow-ups.Just Attila Foris Dec 17, 2025 Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand, measure signal, fit a curve. Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves nothing like the idealized systems we learned in textbooks. GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry and time. The result is a recurring pattern across programs—clean data that is not actually telling the truth. Orthosteric bi Terry's Desk Dec 16, 2025

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Dinner 2 Date & Time Friday, November 3rd / 7:00 PM Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule G Proteins and GPCRs in Cancer: Novel Precision Targeted and Immunotherapies Date & Time Friday, November 3rd / 3:30 PM Abstract Coming Soon About J. Silvio Gutkind "Dr. Gutkind is a Distinguished Professor and Chair of the Department of Pharmacology, School of Medicine, and Associate Director for Basic Science at the Moores Cancer Center, University of California San Diego (UCSD). He served as Branch Chief at NIDCR, NIH, since 1998 until his recruitment to UCSD in 2015. His research team has pioneered the study of G proteins and G protein coupled receptors (GPCRs) in human malignancies. He is exploiting the emerging information on dysregulated signaling circuitries and individual genomic and molecular alterations to develop new precision cancer treatments, and to identify novel multimodal strategies to enhance the response to cancer immunotherapies." J. Silvio Gutkind on the web Gutkind Lab – UC San Diego Moores Cancer Center Gutkind Lab publications Pubmed LinkedIn Twitter UCSD Moores Cancer Center Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Principles of Pharmacology in Drug Discovery II Dr. Terry Kenakin Get Started Premium Members benefits: - Subscribe and save 25% on every GPCR Course - Early-bird access - Recordings will be available < Back to GPCR courses Watch recording Your Instructor Dr. Terry Kenakin

Explore how chemical probes enable real-time GLP-1R visualization in cells and tissues. Episode 2 reveals new GPCR imaging strategies and tool design insights. Home → Flash News → Visualizing GPCRs in their native environment changes everything Visualizing GPCRs in their native environment changes everything Published on December 2, 2025 Category This week on The Dr. GPCR Podcast , we bring you Episode 2 of our three-part series with Celtarys Research — featuring chemist Dr. Johannes Broichhagen , whose work is redefining how we image GPCRs in real tissue. His team’s chemical probes enabled high-resolution GLP-1R visualization across systems — from pancreatic islets to in vivo two-photon imaging. Inside the episode: Chemical probes vs antibodies: specificity, stability, and live-cell performance Mapping GPCR surface pools with precision Tissue-level insights reshaping metabolic disease research What’s next: multiplex receptor labeling + AI-designed tools If GLP-1R biology, receptor trafficking, or advanced imaging are part of your work, this conversation belongs on your radar. 🎧 Listen to Episode 2 → https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/chemical-probes-for-gpcr-imaging-and-internalization And stay tuned for Episode 3 with Celtarys. #GPCR #DrGPCR #metabolism #GLP1R #receptorbiology #fluorescenceimaging #drugdiscovery Previous Next Recent Articles Why Biotech Fundraising Fails Due to Intellectual Property Gaps 👉 Why has intellectual property become a first-order fundraising signal? Biotech fundraising has undergone a subtle yet significant shift. Capital still exists, but investors are making decisions earlier and filtering more carefully . As a result, intellectual property is no longer something that comes up late in the process. 👉 It has become an early signal of whether a biotech company is fundable at all. This shift does not mean founders need more patents or heavier legal Attila Foris 5 days ago The Hidden Operating Cadence That’s Actually Driving Your Biotech Founders love the idea that a new year, or a new quarter, will reset the company. But here’s the uncomfortable truth: 👉 Your biotech is already running on an operating cadence you didn’t consciously design. And that cadence is shaping everything: timelines, decisions, investor calls, BD traction, internal focus. Most CEOs think they’re steering the strategy. 👉 In reality, their operating cadence is steering them. And until you see it, you can’t change it. Operating cadence Attila Foris Dec 24, 2025 GPCR Binding Affinity Experiments: Interpreting Data With Confidence as We Head Into 2026 As scientists, we know curves don’t equal clarity. As 2025 comes to a close, this final edition of Weekly News focuses on how GPCR binding affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development timelines long before anyone notices. The goal isn’t more data. It’s cleaner interpretation. And that’s exactly what carries strong discovery programs into 2026. Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift You Don’t Feel Until It’s Too Late 👉 Every early-stage biotech reaches a moment where the science finally starts clicking… and the company quietly stops doing anything else. BD conversations stay warm but motionless. Investor updates become thinner. Internal meetings slowly morph into scientific colloquia instead of decision-making forums. 👉 The uncomfortable truth: your company is doing a lot of science and very little building. No drama. No blow-ups.Just Attila Foris Dec 17, 2025 Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand, measure signal, fit a curve. Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves nothing like the idealized systems we learned in textbooks. GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry and time. The result is a recurring pattern across programs—clean data that is not actually telling the truth. Orthosteric bi Terry's Desk Dec 16, 2025

Home → Flash News → 🔥 New Course Alert! “Development of GPCR Ligands as Therapeutic Drugs” with Dr. Terry Kenakin is here! Spots are filling up fast—Premium Members get 25% off! This advanced course is exclusively available in the Ecosystem, so don’t miss your chance to learn from the best. 🔹 Secure your spot now! 👉 https://www.ecosystem.drgpcr.com/event-details-registration/development-of-gpcr-ligands-as-therapeutic-drugs #gpcr #drgpcr #pharmacolgy #drugdiscovery #research Published on February 24, 2025 Category Dr. GPCR Courses 🔥 New Course Alert! “Development of GPCR Ligands as Therapeutic Drugs” with Dr. Terry Kenakin is here! Spots are filling up fast—Premium Members get 25% off! This advanced course is exclusively available in the Ecosystem, so don’t miss your chance to learn from the best. 🔹 Secure your spot now! 👉 https://www.ecosystem.drgpcr.com/event-details-registration/development-of-gpcr-ligands-as-therapeutic-drugs #gpcr #drgpcr #pharmacolgy #drugdiscovery #research Previous Next Recent Articles Why Biotech Fundraising Fails Due to Intellectual Property Gaps 👉 Why has intellectual property become a first-order fundraising signal? Biotech fundraising has undergone a subtle yet significant shift. Capital still exists, but investors are making decisions earlier and filtering more carefully . As a result, intellectual property is no longer something that comes up late in the process. 👉 It has become an early signal of whether a biotech company is fundable at all. This shift does not mean founders need more patents or heavier legal Attila Foris 5 days ago The Hidden Operating Cadence That’s Actually Driving Your Biotech Founders love the idea that a new year, or a new quarter, will reset the company. But here’s the uncomfortable truth: 👉 Your biotech is already running on an operating cadence you didn’t consciously design. And that cadence is shaping everything: timelines, decisions, investor calls, BD traction, internal focus. Most CEOs think they’re steering the strategy. 👉 In reality, their operating cadence is steering them. And until you see it, you can’t change it. Operating cadence Attila Foris Dec 24, 2025 GPCR Binding Affinity Experiments: Interpreting Data With Confidence as We Head Into 2026 As scientists, we know curves don’t equal clarity. As 2025 comes to a close, this final edition of Weekly News focuses on how GPCR binding affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development timelines long before anyone notices. The goal isn’t more data. It’s cleaner interpretation. And that’s exactly what carries strong discovery programs into 2026. Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift You Don’t Feel Until It’s Too Late 👉 Every early-stage biotech reaches a moment where the science finally starts clicking… and the company quietly stops doing anything else. BD conversations stay warm but motionless. Investor updates become thinner. Internal meetings slowly morph into scientific colloquia instead of decision-making forums. 👉 The uncomfortable truth: your company is doing a lot of science and very little building. No drama. No blow-ups.Just Attila Foris Dec 17, 2025 Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand, measure signal, fit a curve. Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves nothing like the idealized systems we learned in textbooks. GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry and time. The result is a recurring pattern across programs—clean data that is not actually telling the truth. Orthosteric bi Terry's Desk Dec 16, 2025

Home → Flash News → A complete profile = a complete YOU. Highlight your publications, skills, and interests to connect with the right people! ✳️Go to https://www.ecosystem.drgpcr.com/account/my-account and update your profile on the Dr.GPCR. #gpcr #drgpcr Published on February 5, 2025 Category Dr. GPCR Profiles A complete profile = a complete YOU. Highlight your publications, skills, and interests to connect with the right people! ✳️Go to https://www.ecosystem.drgpcr.com/account/my-account and update your profile on the Dr.GPCR. #gpcr #drgpcr Previous Next Recent Articles Why Biotech Fundraising Fails Due to Intellectual Property Gaps 👉 Why has intellectual property become a first-order fundraising signal? Biotech fundraising has undergone a subtle yet significant shift. Capital still exists, but investors are making decisions earlier and filtering more carefully . As a result, intellectual property is no longer something that comes up late in the process. 👉 It has become an early signal of whether a biotech company is fundable at all. This shift does not mean founders need more patents or heavier legal Attila Foris 5 days ago The Hidden Operating Cadence That’s Actually Driving Your Biotech Founders love the idea that a new year, or a new quarter, will reset the company. But here’s the uncomfortable truth: 👉 Your biotech is already running on an operating cadence you didn’t consciously design. And that cadence is shaping everything: timelines, decisions, investor calls, BD traction, internal focus. Most CEOs think they’re steering the strategy. 👉 In reality, their operating cadence is steering them. And until you see it, you can’t change it. Operating cadence Attila Foris Dec 24, 2025 GPCR Binding Affinity Experiments: Interpreting Data With Confidence as We Head Into 2026 As scientists, we know curves don’t equal clarity. As 2025 comes to a close, this final edition of Weekly News focuses on how GPCR binding affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development timelines long before anyone notices. The goal isn’t more data. It’s cleaner interpretation. And that’s exactly what carries strong discovery programs into 2026. Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift You Don’t Feel Until It’s Too Late 👉 Every early-stage biotech reaches a moment where the science finally starts clicking… and the company quietly stops doing anything else. BD conversations stay warm but motionless. Investor updates become thinner. Internal meetings slowly morph into scientific colloquia instead of decision-making forums. 👉 The uncomfortable truth: your company is doing a lot of science and very little building. No drama. No blow-ups.Just Attila Foris Dec 17, 2025 Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand, measure signal, fit a curve. Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves nothing like the idealized systems we learned in textbooks. GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry and time. The result is a recurring pattern across programs—clean data that is not actually telling the truth. Orthosteric bi Terry's Desk Dec 16, 2025

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Home → Flash News → In case you haven’t heard, registrations are open for the next 4-week course “Development of GPCR Ligands as Therapeutic Drugs,” with Dr. Terry Kenakin 👏 Spots are filling up fast, run and save yours, and enjoy a 25% discount with your Premium Membership 🚀 ✳️Go to https://www.ecosystem.drgpcr.com/event-details-registration/development-of-gpcr-ligands-as-therapeutic-drugs #gpcr #drgpcr Published on February 22, 2025 Category Dr. GPCR Courses In case you haven’t heard, registrations are open for the next 4-week course “Development of GPCR Ligands as Therapeutic Drugs,” with Dr. Terry Kenakin 👏 Spots are filling up fast, run and save yours, and enjoy a 25% discount with your Premium Membership 🚀 ✳️Go to https://www.ecosystem.drgpcr.com/event-details-registration/development-of-gpcr-ligands-as-therapeutic-drugs #gpcr #drgpcr Previous Next Recent Articles Why Biotech Fundraising Fails Due to Intellectual Property Gaps 👉 Why has intellectual property become a first-order fundraising signal? Biotech fundraising has undergone a subtle yet significant shift. Capital still exists, but investors are making decisions earlier and filtering more carefully . As a result, intellectual property is no longer something that comes up late in the process. 👉 It has become an early signal of whether a biotech company is fundable at all. This shift does not mean founders need more patents or heavier legal Attila Foris 5 days ago The Hidden Operating Cadence That’s Actually Driving Your Biotech Founders love the idea that a new year, or a new quarter, will reset the company. But here’s the uncomfortable truth: 👉 Your biotech is already running on an operating cadence you didn’t consciously design. And that cadence is shaping everything: timelines, decisions, investor calls, BD traction, internal focus. Most CEOs think they’re steering the strategy. 👉 In reality, their operating cadence is steering them. And until you see it, you can’t change it. Operating cadence Attila Foris Dec 24, 2025 GPCR Binding Affinity Experiments: Interpreting Data With Confidence as We Head Into 2026 As scientists, we know curves don’t equal clarity. As 2025 comes to a close, this final edition of Weekly News focuses on how GPCR binding affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development timelines long before anyone notices. The goal isn’t more data. It’s cleaner interpretation. And that’s exactly what carries strong discovery programs into 2026. Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift You Don’t Feel Until It’s Too Late 👉 Every early-stage biotech reaches a moment where the science finally starts clicking… and the company quietly stops doing anything else. BD conversations stay warm but motionless. Investor updates become thinner. Internal meetings slowly morph into scientific colloquia instead of decision-making forums. 👉 The uncomfortable truth: your company is doing a lot of science and very little building. No drama. No blow-ups.Just Attila Foris Dec 17, 2025 Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand, measure signal, fit a curve. Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves nothing like the idealized systems we learned in textbooks. GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry and time. The result is a recurring pattern across programs—clean data that is not actually telling the truth. Orthosteric bi Terry's Desk Dec 16, 2025

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Coffee Break 3 Date & Time Friday, November 3rd / 10:25 AM Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Session IV AGPCRs signaling in the nervous system BAI1/ADGRB1-mediated Regulation of Mitochondrial Morphology in Axons Joseph Duman Bai1 Is A Novel Neuronal Substrate Of The Psychiatric Risk Kinase TNIK Simeon R. Mihaylov Intricacies Of Complex Assembly And Ligand Interaction In The Adhesion GPCR Latrophilin/Cirl Anne Bormann BAI1/ADGRB1-mediated Regulation of Mitochondrial Morphology in Axons Joseph Duman Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "Tolias, Kimberley F., Departments of Neuroscience and Biochemistry & Molecular Biology, Baylor College of Medicine, Houston, TX 77030" About Joseph Duman "Joseph Duman is an Assistant Professor in the Department of Neuroscience at Baylor College of Medicine, where he studies BAI1's role in the brain and the radiobiology of treatments for brain cancer. He trained at the University of California at Berkeley with John Forte and the University of Washington with Bertil Hille, before joining Kim Tolias' lab at Baylor College of Medicine." Joseph Duman on the web Baylor College of Medicine Kimberley Tolias Lab Bai1 Is A Novel Neuronal Substrate Of The Psychiatric Risk Kinase TNIK Simeon R. Mihaylov Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "Flynn, Helen R.2, Sampedro-Castaneda, Marisol1, Claxton, Suzanne1, Skehel, Mark2, Ultanir, Sila K.1 1Kinases and Brain Development Laboratory, The Francis Crick Institute, UK 2Proteomics Science Technology Platform, The Francis Crick Institute, UK" About Simeon R. Mihaylov " I am a postdoctoral researcher in the kinases and brain development laboratory led by Dr Sila Ultanir at the Francis Crick Institute in London, England. I undertook my BSc in Biochemistry and Genetics at the University of Sheffield followed up by obtaining a PhD in molecular neuroscience at the Sheffield Institute for Translational Neuroscience. I then moved to King's College London, where my interest and passion for kinases in brain health and disease developed. I initially worked on mTOR in the pathogenesis of Tuberous Sclerosis Complex and then moved to the Francis Crick Institute working on the psychiatric risk kinase TNIK. I also work on multiple other kinases in our laboratory implicated in various neurodevelopmental and neurodegenerative disorders. My expertise includes biochemical approaches, proteomics and transcriptomics to name a few. I have recently also developed a strong interest in adhesion GPCRs and in particular, Bai1. " Simeon R. Mihaylov on the web Crick LinkedIn X (Twitter) Google Scholar Intricacies Of Complex Assembly And Ligand Interaction In The Adhesion GPCR Latrophilin/Cirl Anne Bormann Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "Körner, Marek Benjamin; Dahse, Anne-Kristin; Ljaschenko, Dmitrij; Scholz, Nicole (Rudolf Schönheimer Institute of Biochemistry, Division of General Biochemistry, Faculty of Medicine, Leipzig University)" About Anne Bormann "I am a biochemist by training and studied at Leipzig University from 2015 to 2020. During my Bachelor's in 2018, I sought practical lab experience and found a position as a student assistant in Dr. Nicole Scholz's lab. My main topics were protein biochemistry, Drosophila husbandry, and genetics. I was fortunate that Nicole offered me an opportunity to do my Master's and later on a PhD thesis in her group. Since then, I have broadened my horizons with many more techniques in vivo and in vitro, with a main emphasis on the Adhesion GPCR Latrophilin/Cirl. Currently, I am in the final stages of my PhD, and I am looking forward to new projects and ideas." Anne Bormann on the web Rudolf-Schönheimer-Institut für Biochemie Scholz Lab < Previous Session Next Session >

Join the forefront of GPCR research at the Dr. GPCR Summit! Embracing innovation and technology, we connect global scientific communities. Experience talks spanning time zones, with options for live or pre-recorded presentations. Uncover groundbreaking insights in GPCR science together. Learn more. Meet Dr. GPCR Summit Partners - Click to Explore - Dr. GPCR Summit 2021 Welcome to the official page of the Dr. GPCR Virtual Summit 2021! << Live talk schedule >> << Pre-recorded talk list >> The program is complete! Don't miss a chance to listen to 25+ scientific talks, which will only be available for those who registered during the Summit. Get your All-Access ticket before they're gone by visiting Eventbrite today! Got your All-Access ticket already? Special shout out to our partners! Check your inbox this week, you'll be able to invite a friend or colleague to join the Summit for Free! Proceeds from the ticket sales will be used to provide the best three trainee talks with fantastic prizes, including a personalized autographed copy of Dr. Lefkowitz's biography. Present a pre-recorded talk and get free access to the entire Summit! Hurry, the deadline to submit your talk is Friday, September 10th, 2021, at midnight EST. If you're facing financial difficulties or are a trainee who would like to attend but can't submit a pre-recorded talk, reaches out to us now! The live talks will be held on Zoom, and everyone who registered will be able to ask their questions to the speakers all week on Microsoft Teams! You'll also be able to meet our partners on Microsoft Teams. Make sure you have a profile picture set for both Zoom and Microsoft Teams! Everyone is welcome to present their work (students, postdocs, PI's, biotech, pharma companies)! There are no posters! All pre-recorded talks will be available during the summit for free with registration. All live talks will have a $5 attendance fee/ talk You can get full access to all the talks for $100 For Speakers Step 1: Let us know that you'd like to present your work by filling out this short form here Step 2: Prepare your video abstract and your presentation (pre-recorded or live)* Step 3: Click here to send us your pre-recorded presentation or click here*** to submit the information to your live presentation before August 5th, 2021. ***All live talks are now scheduled Please provide us with your pre-recorded presentation by September 10th, 2021 *Note: Scroll down to find resources to help you prepare your video presentation, and don't hesitate to get in touch if you need help. Contact us at Hello@DrGPCR.com Some housekeeping items first We strongly suggest you carefully consider what type of information you share in your presentation. We will do our best to keep the Summit a closed event, but Dr.GPCR is not responsible for any loss of intellectual property. How will I access the talks during the Summit? You will receive an email from Eventbrite containing the relevant information before the summit. Be sure to register. How can I sponsor the 2021 Summit? Please visit our Sponsor Page to learn more about sponsorship opportunities to sponsor the Summit and the DrGPCR Ecosystem. For more information, please email us at Hello@DrGPCR.com In what form can I submit my abstract? Abstract submission can be in the form of classical text abstract or in the form of a short (max. 3 minutes) video. This is an excellent opportunity to be as creative as you want to be. We recommend writing a 200-300 word abstract, giving you enough information to provide a great video abstract in under 3 minutes. How will I present my talk? You can pre-record your talk. We recommend submitting pre-recorded talks. What does this mean? You send us the video of your full-length talk, and we will take care of the rest. Alternatively, you can provide us with the embed code to make your presentation available during the Summit. Pros: You can polish your recording to your satisfaction. Anyone can watch it from anywhere, even multiple times. Imagine binge-watching your favorite talk over and over whenever you want to during the Summit. Cons: It may take more time to record an excellent presentation, but nothing is impossible! Click here to submit your pre-recorded presentation. Can I present a live talk or event? How? In case you'd like to present a talk live, we'll help with it. Pros: It may take less time to prepare for the presentation Cons: You may make mistakes since it's a live event, and if you decide to keep your talk live only, participants can watch it only once. *Tip Become a DR. GPCR Member by creating your own personalized page. Read more about becoming a member here . If you need help preparing your pre-recorded video and video abstract check out these resources: How to record your talk in PowerPoint 365 How to record your talk using a previous PowerPoint version How to record your talk using Keynote on a Mac Do you have any questions? Email us at Hello@DrGPCR.com << Live talk schedule >> << Pre-recorded talk list >> Meet Dr. GPCR Summit Partners - Click to Explore - Tags Dr. GPCR Summit Dr. GPCR Summit 2021 Dr. GPCR Summit 2021 Pre-Recorded Talks Dr. GPCR Summit 2021 Live Talks

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Complimentary Reception dinner MENU Four Mushroom Soup Tomato, Panela Cheese, and Spinach tower with Oregano Vinaigrette Cane Sugar and Arbol Chile Lacquered Duck Monte Cristo Chocolate Cake Coffee or Tea Vegetarian option* -Mushroom-stuffed chiles on refried bean sauce- instead of the duck < Previous Session Next Session >

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Mexico City Nocturnal Tour, Food and drinks Coming Soon < Previous Session Next Session >

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Posters Interrogating The Role Of CELSR1 (ADGRC1) In Breast Cancer Caroline Formstone Generation and characterization of collecting duct specific GPR56 knockout mice Jianxiang Xue Anti-Tumorigenic Role of Brain Angiogenesis Inhibitor 3 (BAI3) in WNT-Activated Medulloblastomas Virginea de Araujo Farias Conformational And Functional Coupling Between Extracellular and Transmembrane Regions of a Holo-Adhesion GPCR Szymon P. Kordon Deorphanization Of The Adhesion GPCRs GPR110 and GPR116 Tingzhen Shen Self-Cleavage of GPR110 SEA Domain and Its Impact on GAIN Domain Autoproteolysis Bill Huang Tethered Agonist Dependent ADGRL3 Signaling Activity In The G12/13 Pathway Júlia Rosell Endocytic Cues Determine the Signaling Profile of Adhesion GPCR ADGRL1 / Latrophilin-1 Sheila Ribalta-Mena GPR110 modulates anxiety-like behaviors and memory function in mice potentially through neuronal and neuroimmune alterations during neurodevelopment Mariam Melkumyan Interrogating The Role Of CELSR1 (ADGRC1) In Breast Cancer Caroline Formstone Abstract "Breast cancer is the most common form of cancer amongst women. Ductal carcinomas are increasingly diagnosed but identifying which will progress to invasive disease remains difficult highlighting an urgent need for new biomarkers that distinguish ductal carcinomas on this basis. Planar cell polarity (PCP) proteins contribute to tumour growth and invasion. Recent studies identify CELSR1, a key PCP gene, as a novel biomarker for early-stage breast cancer. CELSR1 is reactivated in luminal-type ductal carcinomas. The impact of CELSR1 on cancer progression, however, is unclear. Our working hypothesis is that distinct CELSR1 protein isoforms differentially regulate tissue adhesiveness by influencing the stability/plasticity of cell-cell and cell-matrix contacts. Notably, our pilot data from luminal-type breast cancer cell lines representative of breast carcinomas with lower versus higher invasive potential reveal differential enrichment of CELSR1 protein isoforms. To test the specific hypothesis that biased expression of CELSR1 isoforms will predict invasive potential of a luminal breast carcinoma we will (a) determine, via loss-of-function assays in vitro and in vivo, whether CELSR1 protein isoforms differentially influence the stability of cell-cell and/or cell-matrix adhesions to dictate breast tumour invasive mechanism (b) quantify CELSR1 isoform expression (mRNA and protein) within patient luminal carcinoma samples exhibiting non-invasive or invasive features, the latter including heterogeneous tumours with mixed pathology. Through study of known protein isoforms of CELSR1, which would be missed in gene expression microarray analyses, we hope to illuminate the prognostic potential of CELSR1 for early-stage breast cancer." Authors & Affiliations "Klena, Ladislav University of Hertfordshire" About Caroline Formstone "Cell and developmental biologist with a focus on how planar cell polarity drives complex tissue morphogenesis. I study the cell and tissue level consequences of its failure in foetal development and of its reemployment in cancer" Caroline Formstone on the web University of Hertfordshire Generation and characterization of collecting duct specific GPR56 knockout mice Jianxiang Xue Abstract "GPR56 is a multifunctional adhesin G protein-coupled receptor involved in diverse biological processes. The role of GPR56 in the kidneys has been understudied. A recent study demonstrated that GPR56 in the glomerular endothelial cells promoted diabetic kidney disease progression via regulation of eNOS. Using RNAscope in situ hybridization (ISH) for GPR56, aquaporin 2 and NKCC2 (thick ascending limb, TAL marker), we detected GPR56 mRNA highly expressed in the collecting duct and TAL of the loop of Henle with limited expression in the proximal tubule. To determine the physiological role of GPR56 in the collecting duct, we generated a collecting duct-specific GPR56 knockout (GPR56CD-KO) mouse model by crossing GPR56flox (Control) with cadherin 16 Cre mice. The deletion of GPR56 in the collecting duct was confirmed by RNAscope ISH. GPR56CD-KO mice were born at predicted Mendelian frequencies, appeared grossly indistinguishable from Con mice, and developed normally. For baseline phenotypic characterization, blood gas analysis showed no differences in blood pH, blood HCO3-, blood Na+, or blood K+ between GPR56CD-KO and control mice. Metabolic cage experiments demonstrated no differences in fluid intake, urine volume, urinary pH or urine osmolality between genotypes in baseline. 24hr water deprivation experiment showed that GPR56CD-KO mice can concentrate urine as effectively as control mice. In conclusion, we successfully generated collecting duct-specific GPR56 knockout mouse and found no defective urine concentrating ability in GPR56CD-KO mice. This mouse model will be useful to delineate the collecting duct-specific role of GPR56 for renal function, including acid-base regulation." Authors & Affiliations "Hailey Steichen, Krystin Eaton, Teagan Yan, and Nathan Zaidman; Department of Biochemistry and Molecular Biology, University of New Mexico" About Jianxiang Xue "I am a postdoctoral researcher working in the Department of Biochemistry and Molecular Biology, University of New Mexico. I earned my PhD degree in Biomedical Sciences from the University of South Florida. During my graduate studies, using various transgenic mouse models and expertise in intestinal and renal physiology, I systematically characterized the function of sodium/hydrogen exchanger 3 in the intestine and kidneys for fluid and electrolyte homeostasis and acid-base balance. My predoctoral work was supported by an American Heart Association fellowship. Since staring my postdoctoral training, I have continued to develop my expertise to answer fundamental questions on adhesion GPCR in renal physiology and pathology. In my free time, I enjoy reading, workouts, and hiking." Jianxiang Xue on the web Zaidman Physiology Lab Anti-Tumorigenic Role of Brain Angiogenesis Inhibitor 3 (BAI3) in WNT-Activated Medulloblastomas Virginea de Araujo Farias Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Van Meir, Erwin G. University of Alabama at Birmingham" About Virginea de Araujo Farias "Brain Angiogenesis Inhibitor (BAI) proteins are members of group VII of the adhesion G protein-coupled receptor (aGPCR) family. BAI1-3 are highly expressed in the brain, where they participate in synaptogenesis and synapse maintenance. In cancers, BAI1-3 expression can be lost through epigenetic silencing, copy number loss or truncating mutations. In medulloblastomas (MB), BAI3 (ADGRB3) expression is specifically reduced in the WNT-activated group (WNT-MB), but not in the other three molecular groups. WNT pathway activation in WNT-MB is driven by mutations of the CTNNB1 gene, activating ß-catenin-dependent signaling; however, no interactions between BAI3 and the WNT signaling pathway have been described so far. MAGI3, a PDZ-containing scaffolding protein is known to downregulate WNT signaling by interacting with ß-catenin in gliomas, but it is unknown whether this involves BAI3. To explore a possible connection between BAI3 and ß-catenin signaling through MAGI3 in WNT-MB, we probed for potential protein-protein interactions using co-IP experiments. We found an interaction between BAI3 and MAGI3 in mouse brain lysates. Therefore, we hypothesize that re-expression of BAI3 in WNT-MB cells will restrain ß-catenin activity through the formation of a BAI3/MAGI3/ß-catenin complex, reducing their tumorigenic properties. To test this hypothesis, we created WNT-like MB cell lines stably expressing tet-on wild-type BAI3 or a BAI3 lacking the C-terminal PDZ-binding motif (PBM). We will present the effects of BAI3 re-expression on WNT-MB cells oncogenic properties and signaling." Virginea de Araujo Farias on the web Google Scholar Conformational And Functional Coupling Between Extracellular and Transmembrane Regions of a Holo-Adhesion GPCR Szymon P. Kordon Abstract "Adhesion G Protein-Coupled Receptors (aGPCRs) are key cell-adhesion molecules involved in numerous physiological functions. aGPCRs have large multi-domain extracellular regions (ECR) that mediate cell adhesion and play roles in transmitting extracellular signals to the inside of the cell. Ligand binding and mechanical force applied on the ECR regulate receptor function. However, how the ECR communicates with the seven-pass transmembrane domain (7TM) remains elusive, because the relative orientation and dynamics of the ECR and 7TM within a holoreceptor is unclear. Here, we describe the cryo-EM reconstruction of an aGPCR, Latrophilin3/ADGRL3, and reveal that the conserved GAIN domain, that directly precedes 7TM, adopts a parallel orientation to the membrane and has constrained movement. Single-molecule FRET experiments unveil three slow-exchanging FRET states of the ECR relative to the 7TM within the holoreceptor. GAIN-targeted antibodies, and cancer-associated mutations at the GAIN-7TM interface, alter holoreceptor conformations, and modulate downstream receptor signaling. Altogether, this data demonstrates conformational and functional coupling between the ECR and 7TM, suggesting an ECR-mediated mechanism for aGPCR activation." Authors & Affiliations "Cechova Kristina (3), Bandekar Sumit J.(1, 2), Leon Katherine (1, 2), Dutka Przemysław (1, 4), Siffer Gracie (3), Kossiakoff Anthony A. (1), Vafabakhsh Reza (3), Araç Demet (1, 2) 1. Department of Biochemistry and Molecular Biology, The University of Chicago, Chicago, IL, USA; 2. Neuroscience Institute, Institute for Biophysical Dynamics, and Center for Mechanical Excitability, The University of Chicago, Chicago, IL, USA; 3. Department of Molecular Biosciences, Northwestern University, Evanston, IL, USA; 4. Current affiliation: Department of Structural Biology, Genentech, South San Francisco, CA, USA" About Szymon P. Kordon "I am a postdoctoral scholar in the Araç Lab at The University of Chicago, studying the structure and function of aGPCRs. Utilizing synthetic antibody fragments, I aim to understand better the structural basis of the aGPCRs activation and signaling and to characterize ECR-mediated signal transduction at the molecular level." Szymon P. Kordon on the web Araç Laboratory at UChicago Deorphanization Of The Adhesion GPCRs GPR110 and GPR116 Tingzhen Shen Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Frank E. Kwarcinski, Gregory G. Tall (University of Michigan, Ann Arbor)" About Tingzhen Shen "A graduate student from Tall Lab, department of Pharmacology, University of Michigan, Ann Arbor." Tingzhen Shen on the web University of Michigan Self-Cleavage of GPR110 SEA Domain and Its Impact on GAIN Domain Autoproteolysis Bill Huang Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Hee-Yong Kim, Laboratory of Molecular Signaling, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Rockville, MD, USA" About Bill Huang "Researcher" Bill Huang on the web LinkedIn Tethered Agonist Dependent ADGRL3 Signaling Activity In The G12/13 Pathway Júlia Rosell Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Regmi, Rajesh (1), Perry-Hauser, Nicole A. (2), Javitch, Jonathan A. (2), Mathiasen, Signe (1) (1) Department of Biomedical Sciences, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark. (2) Department of Psychiatry and Molecular Pharmacology and Therapeutics, Columbia University Vagelos College of Physicians and Surgeons, New York, USA; Division of Molecular Therapeutics, New York State Psychiatric Institute, New York, USA" About Júlia Rosell "I am a first-year PhD student with two years of experience in the adhesion GPCR field. I completed my Master’s thesis on ADGRL3, where I conducted research involving mammalian cell cultures and techniques such as BRET assays and gene expression assays. Currently, my research focuses on the intracellular signaling of ADGRL3 from a single-molecule perspective and investigating how the binding of extracellular transsynaptic ligands modulates ADGRL3 activity, aiming to elucidate their interplay." Júlia Rosell on the web LinkedIn Endocytic Cues Determine the Signaling Profile of Adhesion GPCR ADGRL1 / Latrophilin-1 Sheila Ribalta-Mena Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations " Hernández-Aranda Judith 2, Correoso-Braña Kerlys 1, Vialou Vincent 3, Leduc Richard 4, Olivares-Reyes Jesús Alberto 2, Boucard Antony A1. 1 Department of Cell Biology, Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional (Cinvestav-IPN), México City, México. 2 Department of Biochemistry, Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional (Cinvestav-IPN), México City, México. 3 Sorbonne Université, Inserm, CNRS, Neurosciences Paris Seine, Paris, France. 4 Department of Physiology and Pharmacology, Université de Sherbrooke, Sherbrooke, Canada " About Sheila Ribalta-Mena " Cell Biology PhD student " Sheila Ribalta-Mena on the web CINVESTAV ResearchGate LinkedIn GPR110 modulates anxiety-like behaviors and memory function in mice potentially through neuronal and neuroimmune alterations during neurodevelopment Mariam Melkumyan Abstract "GPR110, an adhesion G protein coupled receptor (GPCR), is widely expressed in developing brains but diminishes in adult stage except in the hippocampus, a region involved in learning and memory. Ligand-induced GPR110 signaling stimulates neurogenesis and synaptogenesis during development, and the absence of the ligand-induced signaling causes object recognition and spatial memory deficits in adulthood and increased neuroinflammatory responses. Nevertheless, the role of GPR110 signaling in behavioral consequences has not been fully explored. This study aimed to understand the effects of GPR110 on mouse behaviors in relation to neurodevelopmental and neuroimmune gene and protein expression. Anxiety and memory function were tested using both male and female mice at 5-6 month of age. GPR110 knockout (KO) mice displayed trends for increased anxiety-like behaviors in the elevated plus maze test and in the open field test. Memory tests, including the novel object test and the radial 8-arm maze showed worsened spatial and reference memory in the GPR110 KO mice compared to wildtype mice. The y-maze showed a significant sex by genotype interactions with GPR110 KO male mice having increased number of correct alterations and errors, while the GPR110 KO females had fewer correct alterations and errors. RNAseq data indicated significantly impaired developmental gene expression for neuronal differentiation, axonogenesis, and synaptogenesis, as well as altered neuroinflammatory marker expression in GPR110 KO mouse brains. Further studies exploring the protein expression and neural activity of these mouse brain will give insight on the mechanism underlying the behavioral consequences associated with the GPR110 receptor. " Authors & Affiliations "Joel Toro, Bill Huang, Hee-Yong Kim Laboratory of Molecular Signaling, National Institute of Alcohol Abuse and Alcoholism, NIH" About Mariam Melkumyan "Mariam Melkumyan is a postdoctoral fellow at the Laboratory of Molecular Signaling studying the role of GPR110 in neurotransmission and neuroimmune activity involved in learning and memory, anxiety, and alcohol use. Mariam, originally from Armenia, completed her bachelor's degree in Neuroscience at American University in Washington, DC and her dual-title PhD in Neuroscience and Clinical and Translational Sciences at Penn State College of Medicine in Hershey, PA. Mariam started her postdoctoral training in February 2024 and is hoping to become an academic professor and mentor the next generation of scientists." Mariam Melkumyan on the web LinkedIn Google Scholar < Previous Session Next Session >

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Closing remarks < Previous Session Next Session >

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Session VIII Physiological and pathological roles of AGPCRs in the periphery ADGRG1/GPR56 regulates survival of terminally differentiated CD8+ T cells Cheng-Chih Hsiao Adhesion GPCR GPR116/Adgrf5 controls a lineage of anti-thermogenic adipocytes with implications for adaptive thermogenesis during prolonged cold exposure Anastasia Georgiadi ADGRF5-mediated regulation of cardiac health and disease Douglas Tilley ADGRG1/GPR56 regulates survival of terminally differentiated CD8+ T cells Cheng-Chih Hsiao Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "Cheng-Chih Hsiao1,2, Hendrik J. Engelenburg1, Joost Smolders1,3, and Jörg Hamann1,2 1Department of Neuroimmunology, Netherlands Institute for Neuroscience, Amsterdam, The Netherlands; 2Department of Experimental Immunology, Amsterdam institute for Immunology and Infectious diseases, Amsterdam University Medical Center, Amsterdam, The Netherlands; 3MS center ErasMS, Departments of Neurology and Immunology, Erasmus Medical Center, Rotterdam, The Netherlands" About Cheng-Chih Hsiao "2012-2015: PhD in Immunology, University of Amsterdam; 2015-2019: Postdoctoral researcher, Amsterdam UMC; 2019-2022: Senior postdoctoral researcher, Netherlands Institute for Neuroscience; 2022 - present: Researcher associate, Netherlands Brain Bank" Cheng-Chih Hsiao on the web LinkedIn ReseachGate Adhesion GPCR GPR116/Adgrf5 controls a lineage of anti-thermogenic adipocytes with implications for adaptive thermogenesis during prolonged cold exposure Anastasia Georgiadi Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "El Merabhi Rabih1*, Karagiannakou Vasiliki1*, Kardinal Ronja2, Jäckstein Michelle3 Yvonne, Kumar Jha Ankush1, Krokidi Sissy Thodou1, Wachten Dagmar2, Heeren Jörg3, Herzig Stephan1, Georgiadi Anastasia1 *equal contributions , Institutions : 1. Institute for Diabetes and Cancer, Helmholtz Centre Munich, Germany, 2. Institute of Innate Immunity, University Hospital Bonn, University of Bonn, 3. Centre for Experimental Medicine, Institute for Biocehmistry and Molecular Cell Biology, University Medical Center Hamburg-Eppendorf" About Anastasia Georgiadi "Head of Junior Group Endocrine Pharmacology, Institute of Diabetes and Cancer (IDC). Professional Background Since 2021 Group Leader, Institute for Diabetes and Cancer, Helmholtz Diabetes Centre, Munich 2018 - 2021 Project Team Leader, Institute for Diabetes and Cancer, Helmholtz Diabetes Centre, Munich 2015 - 2018 Postdoctoral fellow, Department of Adipose Tissue Biology, Institute for Diabetes and Cancer, Helmholtz Diabetes Centre, Munich 2012 - 2015 Postdoctoral fellow, Department of Cell and Molecular Biology, Karolinska Institute, Sweden" Anastasia Georgiadi on the web Endocrine Pharmacology Google Scholar ADGRF5-mediated regulation of cardiac health and disease Douglas Tilley Abstract Only available for AGPCR 24 Attendees About Douglas Tilley "Research in the Tilley laboratory focuses primarily upon aspects of GPCR regulation of cardiac function, inflammation and remodeling during HF or following acute cardiac injury. Much of this work centered on elucidating novel mechanisms by which β-adrenergic receptors impact cardiac structure and function, and has evolved to encompass their roles in regulating immune cell response to acute cardiac injury or chronic stress. Additionally, the lab has begun to investigate potential roles for previously unrecognized cardiac-expressed GPCRs in the regulation of physiologic/pathologic function in the heart in an effort to uncover novel therapeutic directions for HF, including adhesion GPCRs (AGPCRs). In all, research in the Tilley lab spans molecular pharmacology to pathophysiology studies focused primarily in the cardiovascular realm." Douglas Tilley on the web Lewis Katz School of Medicine at Temple University < Previous Session Next Session >

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Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Coffee Break with lights snacks Complimentary < Previous Session Next Session >

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Session VIII * Physiological and pathological roles of AGPCRs in the periphery The CELSR/ADGRC Homolog Flamingo Is Not Autoproteolytically Processed By The GAIN Domain Tobias Langenhan Characterization of Phenotypes Associated with GPR110 Deletion Hee-Yong Kim The Adhesion GPCR Cupidon Regulates Mating In The Closest Relatives Of Animals Alain Garcia De Las Bayonas Critical role for CD97/ADGRE5 in the induction of allergic airway inflammation Gabriela Aust The CELSR/ADGRC Homolog Flamingo Is Not Autoproteolytically Processed By The GAIN Domain Tobias Langenhan Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "Tobias Langenhan, Nicole Scholz, Genevieve M. Auger, Helen Strutt, David Strutt" About Tobias Langenhan "1997-2004: Medical school and Dr. med. Neuroanatomy (Würzburg, Germany); 2004-2005: M.Sc. Neuroscience (Oxford, UK); 2005-2009: D.Phil. Neuroscience (Oxford, UK); 2009-2016: Group leader, Institute of Neurophysiology (Würzburg, Germany); 2016: Heisenberg professorship (Würzburg, Germany); 2016-to date: Professor and Chair in Biochemistry (Leipzig, Germany)" Tobias Langenhan on the web Langenhan Lab LinkedIn Characterization of Phenotypes Associated with GPR110 Deletion Hee-Yong Kim Abstract "G-protein coupled receptor 110 (ADGRF1, GPR110), an adhesion GPCR recently deorphanized, plays an important role in in the development of neurons and cognitive function. Synaptamide, an endogenous ligand for GPR110, binds to the N-terminal G-protein autoproteolysis-inducing (GAIN) domain of GPR110, and activates GPR110/cAMP signaling. This activation promotes neurogenic differentiation of neural stem cells, neurite growth, and synaptogenesis of developing neurons. In addition, a significant role of GPR110 in blood brain barrier (BBB) function has been discovered. GPR110 is highly expressed in mouse and human NPCs and neurons, while its expression was absent in astrocytes. GPR110 is also highly expressed in the kidney, however, little is known about the function of this receptor in renal physiology. To extend our understanding of the role of GPR110 signaling in kidney, we evaluated the urine albumin level in mice devoid of GPR110 gene (GPR110 KO) compared to the wild type (WT). To provide the molecular basis for the renal phenotype, we analyzed in parallel differential expression of kidney proteins in GPR110 KO and WT mice by label-free LC-MS/MS and pathway analysis. We found that the albumin to creatinine ratio was significantly elevated in urine samples obtained from GPR110 KO mice, indicating glomerular filtration dysfunction. The change in protein expression of key proteins including VEGFA is associated with the abnormal renal phenotype of albumin urea in GPR110 KO mice. In addition to the central nervous system phenotype such as learning and memory deficit and BBB dysfunction, our study revealed a new renal phenotype associated with lack of GPR110 signaling. " Authors & Affiliations "Laboratory of Molecular Signaling, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, USA" About Hee-Yong Kim "Senior Investigator and Chief of the Laboratory of Molecular Signaling at NIAAA, NIH" Hee-Yong Kim on the web NIH The Adhesion GPCR Cupidon Regulates Mating In The Closest Relatives Of Animals Alain Garcia De Las Bayonas Abstract "All animals develop through the recognition, adhesion, and fusion of a differentiated sperm and egg. Although fundamental, the evolution of gametogenesis and fertilization in animals is poorly understood. Recently, evidence for sex has been described in choanoflagellates, the closest living relatives of animals. Under nutrient depletion, the model choanoflagellate Salpingoeca rosetta forms distinct cell types that aggregate, fuse, and undergo meiotic recombination. Additionally, the bacterium Vibrio fischeri also induces mating in S. rosetta cultures, suggesting that multiple environmental cues can trigger sex. Importantly, the signaling pathways underlying sexual reproduction in these different contexts have not been investigated. In this study, we report the discovery of an adhesion GPCR, named Cupidon, that regulates the switch from vegetative growth to sexual reproduction in S. rosetta. We found that the knock-out of cupidon induces a gain in cell adhesion and cell fusion, resembling the mating behavior of wild-type cells under nutrient depletion. Cupidon mutants, similar to starved wild-type cells, upregulate various extracellular matrix-related genes, including teneurins and metalloproteases. Finally, we showed that nutrient availability controls the dissociation of the N-terminal fragment in Cupidon. Together, our results suggest that Cupidon prevents sexual reproduction in S. rosetta under high nutrient availability, by inhibiting genes involved in gamete recognition. " Authors & Affiliations "King Nicole, Howard Hughes Medical Institute and Department of Molecular and Cell Biology, University of California Berkeley" About Alain Garcia De Las Bayonas "Hi everyone! I am currently finishing my postoc in the laboratory of Pr Nicole King at UC Berkeley where I am studying the evolution of GPCR families in choanoflagellates, the sister group of animals. I have a particular interest in understanding the premetazoan function of adhesion GPCRs." Alain Garcia De Las Bayonas on the web King Lab Critical role for CD97/ADGRE5 in the induction of allergic airway inflammation Gabriela Aust Abstract Only available for AGPCR 24 Attendees Authors & Affiliations Coming Soon About Gabriela Aust Coming Soon Gabriela Aust on the web Coming Soon < Previous Session Next Session >

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Discover how low-offset kinetics reshape drug efficacy. Join Terry’s Corner and master irreversible pharmacology for modern discovery programs. Home → Flash News → irreversible drugs post 1 Irreversible Drugs – Trailer Published on October 21, 2025 Category Terry's Corner Irreversible drugs change the rules of engagement. Unlike reversible ligands, their impact can persist long after the compound is gone — creating durable pharmacological effects that reshape how pharmacokinetics and pharmacodynamics intersect. In modern discovery programs, that’s a decisive advantage (or a hidden liability) in candidate selection. In this week’s lesson, you’ll unpack: Why low offset rates can mimic covalent effects without forming actual bonds. How target depletion and replenishment kinetics define the therapeutic window. How persistent binding alters structured tissue penetration — and why that matters for tumor targeting and beyond. These tactical frameworks are used to optimize molecules, sharpen PK/PD strategy, and mitigate downstream safety surprises before they appear in IND-enabling studies. Understanding irreversible interactions can mean the difference between a stalled program and a strategic breakthrough. Those who master kinetic pharmacology set the pace. 🟢 Join Terry’s Corner and sharpen your pharmacology toolkit. ✳️ Terry's Corner | Dr. GPCR Ecosystem #GPCR #DrGPCR #Pharmacology #DrugDiscovery #MedicinalChemistry #PKPD #ReceptorKinetics #DrugDevelopment Previous Next Recent Articles Why Biotech Fundraising Fails Due to Intellectual Property Gaps 👉 Why has intellectual property become a first-order fundraising signal? Biotech fundraising has undergone a subtle yet significant shift. Capital still exists, but investors are making decisions earlier and filtering more carefully . As a result, intellectual property is no longer something that comes up late in the process. 👉 It has become an early signal of whether a biotech company is fundable at all. This shift does not mean founders need more patents or heavier legal Attila Foris 5 days ago The Hidden Operating Cadence That’s Actually Driving Your Biotech Founders love the idea that a new year, or a new quarter, will reset the company. But here’s the uncomfortable truth: 👉 Your biotech is already running on an operating cadence you didn’t consciously design. And that cadence is shaping everything: timelines, decisions, investor calls, BD traction, internal focus. Most CEOs think they’re steering the strategy. 👉 In reality, their operating cadence is steering them. And until you see it, you can’t change it. Operating cadence Attila Foris Dec 24, 2025 GPCR Binding Affinity Experiments: Interpreting Data With Confidence as We Head Into 2026 As scientists, we know curves don’t equal clarity. As 2025 comes to a close, this final edition of Weekly News focuses on how GPCR binding affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development timelines long before anyone notices. The goal isn’t more data. It’s cleaner interpretation. And that’s exactly what carries strong discovery programs into 2026. Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift You Don’t Feel Until It’s Too Late 👉 Every early-stage biotech reaches a moment where the science finally starts clicking… and the company quietly stops doing anything else. BD conversations stay warm but motionless. Investor updates become thinner. Internal meetings slowly morph into scientific colloquia instead of decision-making forums. 👉 The uncomfortable truth: your company is doing a lot of science and very little building. No drama. No blow-ups.Just Attila Foris Dec 17, 2025 Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand, measure signal, fit a curve. Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves nothing like the idealized systems we learned in textbooks. GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry and time. The result is a recurring pattern across programs—clean data that is not actually telling the truth. Orthosteric bi Terry's Desk Dec 16, 2025

Home → Flash News → Did you know? 🌟 Researchers have developed reversibly photoswitchable allosteric modulators for Class A GPCRs! 🧬💡 These innovative compounds, “Photo-BQCisA” and “Photo-BQCtrAns,” offer subtype-selective precision by combining allosteric modulation with light control, paving the way for new therapeutic strategies targeting muscarinic receptors (M1-M5). 🔬✨ Learn more about this breakthrough in the Ecosystem! Published on December 3, 2024 Category GPCR Weekly News Did you know? 🌟 Researchers have developed reversibly photoswitchable allosteric modulators for Class A GPCRs! 🧬💡 These innovative compounds, “Photo-BQCisA” and “Photo-BQCtrAns,” offer subtype-selective precision by combining allosteric modulation with light control, paving the way for new therapeutic strategies targeting muscarinic receptors (M1-M5). 🔬✨ Learn more about this breakthrough in the Ecosystem! ➡️ buff.ly/4fgX4ZH #gpcr #drgpcr Previous Next Recent Articles Why Biotech Fundraising Fails Due to Intellectual Property Gaps 👉 Why has intellectual property become a first-order fundraising signal? Biotech fundraising has undergone a subtle yet significant shift. Capital still exists, but investors are making decisions earlier and filtering more carefully . As a result, intellectual property is no longer something that comes up late in the process. 👉 It has become an early signal of whether a biotech company is fundable at all. This shift does not mean founders need more patents or heavier legal Attila Foris 5 days ago The Hidden Operating Cadence That’s Actually Driving Your Biotech Founders love the idea that a new year, or a new quarter, will reset the company. But here’s the uncomfortable truth: 👉 Your biotech is already running on an operating cadence you didn’t consciously design. And that cadence is shaping everything: timelines, decisions, investor calls, BD traction, internal focus. Most CEOs think they’re steering the strategy. 👉 In reality, their operating cadence is steering them. And until you see it, you can’t change it. Operating cadence Attila Foris Dec 24, 2025 GPCR Binding Affinity Experiments: Interpreting Data With Confidence as We Head Into 2026 As scientists, we know curves don’t equal clarity. As 2025 comes to a close, this final edition of Weekly News focuses on how GPCR binding affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development timelines long before anyone notices. The goal isn’t more data. It’s cleaner interpretation. And that’s exactly what carries strong discovery programs into 2026. Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift You Don’t Feel Until It’s Too Late 👉 Every early-stage biotech reaches a moment where the science finally starts clicking… and the company quietly stops doing anything else. BD conversations stay warm but motionless. Investor updates become thinner. Internal meetings slowly morph into scientific colloquia instead of decision-making forums. 👉 The uncomfortable truth: your company is doing a lot of science and very little building. No drama. No blow-ups.Just Attila Foris Dec 17, 2025 Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand, measure signal, fit a curve. Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves nothing like the idealized systems we learned in textbooks. GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry and time. The result is a recurring pattern across programs—clean data that is not actually telling the truth. Orthosteric bi Terry's Desk Dec 16, 2025