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But when Beth Fleck measured dissociation rates of the CRF receptor radioligands, the compound that worked

. << Back to podcast list Strategic Partner(s) Bryan Roth: Inside the DARPA Bet on a Non-Psychedelic The bet is that biased ligands at the serotonin 2A receptor can separate the two. A famous scientist at Stanford and an NIH program officer both told Dr.

traces the accidental origins of his receptor research — from a Vietnam War draft to the cloning of the beta Lefkowitz: Beta-Adrenergic Receptors, the GPCR Family, and Fifty Years of Discovery The existence of Using radioligand binding assays developed for the beta-adrenergic receptor system, his lab purified, The same system yielded the discovery of beta-adrenergic receptor kinase (now GRK2) and the beta-arrestins The strategic logic behind choosing beta-adrenergic receptors The selection of the beta-adrenergic system

Arun Shukla on how two beta-arrestin isoforms regulate over 800 receptors, why "non-canonical" GPCRs information from NMR and hydrogen-deuterium exchange, and custom-engineered antibody fragments that both beta-arrestin-biased receptors Engineered antibody fragments as tools for structural stabilization and Shukla's lab is also one of the field's oldest open questions: how do just two beta-arrestin isoforms Shukla's lab and others have shown they signal robustly through beta-arrestins — which makes them, in

Annette Gilchrist on why native cell systems change GPCR screening, constitutive beta-arrestin activity Whether a 20% reduction in beta-arrestin coupling matters therapeutically depends on the cell type, the That discipline led to a finding her field had not documented before: constitutive beta-arrestin activity framing rarely holds at the clinical level Constitutive beta-arrestin activity and inverse agonism - Is a 20% reduction of beta-arrestin signaling enough? I think it is probably cell-dependent.

wet-lab work stops GPCR density and tissue-specific therapeutic opportunity — type II pneumocytes, beta The lung's beta-2 story has been sitting in plain sight for fifty years. Type II pneumocytes carry the highest beta-2 receptor density in the body. Long-acting beta-agonists paired with glucocorticoids have been the mainstay of asthma treatment for 11:00 Gas pedals and brakes — biology's architecture of opposing forces 14:00 Type II pneumocytes, beta

weren't ready, what it takes to hold a GPCR signaling lab together during a pandemic, and the BRET-based beta work already in the pipeline before the shutdown, including a newly accepted BRET-based platform for beta resonance-energy-transfer-based assays in capturing signaling downstream of specific receptors, with the beta The beta-1 adrenergic receptor paper — a BRET-based platform for capturing downstream signaling, built epicenter 03:06 Paper acceptances, thesis writing, and 30 hours of Zoom teaching in one month 04:29 The beta

Hebert's research focuses on the angiotensin AT1 receptor, a signaling hub coupled to Gq, Gi, G12, and beta-arrestin Beyond the Gq/Beta-Arrestin Dichotomy — The AT1 receptor couples to Gq, Gi, G12, and beta-arrestin simultaneously Defies Simple Classification The angiotensin AT1 receptor is not just a Gq-coupled receptor with a beta-arrestin The goal is to test therapeutic strategies targeting the AT1R, alpha-adrenergic, and beta-adrenergic Hebert's path to GPCRs 03:26 The angiotensin AT1 receptor — a favorite and a mystery 05:05 Why the Gq/beta-arrestin

biased agonism, with the development of approaches to quantify ligand bias and the identification of beta-arrestin-biased signal transduction mechanisms of GPCRs, such as the formation of complexes between G proteins and beta-arrestins

Marshall, the throughline is personal: she remembers the exact lecture at Bath where she first heard The moment baclofen activated ion channels in Xenopus oocytes expressing both — with Dr. mic Selected Quotes "We did the classic experiment in Xenopus oocytes, where you inject the cDNA of both About this episode Fiona Marshall got fascinated with GPCRs after attending a lecture on how the beta-adrenergic receptor in the heart is activated by adrenaline, during her undergraduate studies at Bath University

Beaulieu has pioneered work establishing a role for Beta-arrestin signaling in the brain in vivo and proteins can act as allosteric modulators of D2R signaling and explores the potential usefulness of beta-arrestins

are large, lipid-modified proteins that require carrier molecules for transport, their canonical Wnt–beta-catenin couples to distinct G-protein families in ways that challenge the field's conventional focus on the beta-catenin Disheveled may regulate access to both G-protein and beta-catenin pathways through conformational selection Disheveled (DVL), the scaffolding protein downstream of frizzled, is not simply a beta-catenin pathway frizzled family 34:55 SAG1.3: repurposing a Smoothened compound to activate frizzled 6 40:51 Where beta-arrestin

Current efforts aim to understand the regulation of GPCR and beta-arrestin signaling in the heart and

Annabelle Milner Annabelle completed her undergraduate degree in Biomedical Sciences at the University of Bath

Research in my lab is currently focused on understanding the signal transduction pathways activated by beta-adrenergic

as a postdoctoral fellow and trained on understanding the physiological role of GPCR signaling and beta-arrestins

She trained as a postdoctoral fellow in von Zastrow's lab at UCSF, where she worked on beta-2 adrenergic She describes the shift as both technically disorienting and visually striking - a different relationship from an academic-industry collaboration that would not have produced the allosteric modulators without both lab and the internalization paradigm shift 14:17 How to choose a postdoc with no trial period 19:07 Beta academia stopped making sense 30:54 From Field Application Scientist to Product Manager 38:58 What both

-1997), where he and his colleagues investigated the role of G protein-coupled receptor kinases and beta-arrestin He has also received both Junior (2001) and Senior (2005) investigator awards from the Pharmacological

-1997), where he and his colleagues investigated the role of G protein-coupled receptor kinases and beta-arrestin He has also received both Junior (2001) and Senior (2005) investigator awards from the Pharmacological

G protein-coupled receptor signaling particularly by the G protein-coupled receptor kinase (GRK) – beta-arrestin

G protein-coupled receptor signaling particularly by the G protein-coupled receptor kinase (GRK) – beta-arrestin

G protein-coupled receptor signaling particularly by the G protein-coupled receptor kinase (GRK) – beta-arrestin

G protein-coupled receptor signaling particularly by the G protein-coupled receptor kinase (GRK) – beta-arrestin

His research centers on the beta-2 adrenergic receptor and GPR65 , a proton-sensing receptor with promising This episode is both educational and inspiring, offering a behind-the-scenes look at a rising scientist

spent several years in Switzerland working on the study of membrane trafficking processes in pancreatic beta

his entire research direction. 21 degrees changed what was chemically possible Thermostabilizing the beta-adrenergic The Friday afternoon library paper that changed GPCR structural biology 24:21 Thermostabilizing the beta Chris also worked on the E. coli multidrug transporter EmrE and obtained both 2D and 3D crystals as well

How collaborations with David Parker and Jean-Philippe Pin accelerated both probe chemistry and biological What it felt like to see the first dose-response curves in native beta cells—and why that moment changed

Her current research integrates both frameworks - examining how the GLP-1 receptor engages its transducer A decade later, she is deliberately bringing both ends of that arc together. target profile changes the stakes of understanding how the receptor works - not only in pancreatic beta make asking safe, and by the unavoidable evidence that unacknowledged confusion produces problems on both

unexpected discovery: phospholipids embedded inside each transmembrane bundle that appear to function as both structural work identified a quartet of charged residues - salt bridges between TM3 and TM5 helices of both spectrometry in collaboration with colleagues at UC Davis, they identified the exact molecular identity of both Both lipids form extensive contacts with their respective subunits, leading Fan to propose they are necessary confers analgesia through G protein signaling while avoiding the respiratory depression associated with beta-arrestin

For example, you might take the extracellular and transmembrane domains of the beta-2 adrenergic receptor