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John Streicher: Reorganizing Opioid Signaling Beyond the Receptor The dominant strategy for improving , delta, and kappa opioid receptors. drug design The current state and replication troubles of biased agonism at the mu opioid receptor Downstream In the brain, HSP90 promotes ERK activation downstream of the mu opioid receptor and is required for John Streicher 01:49 From heart failure to opioids — a path through signaling 07:49 Why the mu receptor

Amynah Pradhan on why mu opioids worsen migraine, why delta agonists may relieve it, and how chronic Receptor and the Migraine Paradox Chronic migraine sits at a peculiar crossroads in opioid pharmacology : sustained mu opioid receptor activation is a well-documented driver of medication-overuse headache, Scientific Themes of the Conversation The mu/delta asymmetry in migraine — why two receptors in the same Paul Clarck , where she studied opioid receptors.

glutamate receptors, and the calcium-sensing receptor, the molecular mechanisms governing their activation opioid receptor by Kobilka, Gnäder, Roth, and Shokat as an illustration of what pathway-selective drug A decade on one receptor: the cost and the clarity it produces Fan has worked on the GABA-B receptor precision medicine 19:03 - GPCRs as drug targets: allosteric sites, biased signaling, and what the mu opioid receptor example demonstrated 23:37 - What full-length structures in multiple states still need

journey highlights the transition from general drug development to a deep dive into G protein-coupled receptors on positive allosteric modulators (PAMs) targeting opioid receptors. from the University of Minnesota in 2022, studying the pharmacokinetics and pharmacodynamics of NMDA receptor focuses on determining the mechanisms of action of a series of positive allosteric modulators of the mu-opioid receptor.

Fast, clear, live-cell receptor trafficking detection. This technology supports robust analysis even at low endogenous receptor expression levels. Internalization into acidic compartments = signal activation: Upon receptor-mediated endocytosis, the View Product pHSense Eu SNAP Labeling Reagent Can be used to label receptors and membrane proteins carrying All four formats are validated in well-established models like GLP1R and Mu opioid receptor (MOR), and

The conversation covers why GPCR targets are especially difficult to immunize against, how receptor family development The five-pillar approach to antibody characterization applied to notoriously difficult receptor Chemokine receptors like CXCR1 and CXCR2 share over 75% sequence identity - use the wrong peptide region LGR5 Became GeneTex's Reckoning with the GPCR Target Class LGR5 - a receptor critical to adult stem cell opioid receptor, purchased multiple commercial antibodies, and found that several of them produced signal

Livingston on allosteric opioid modulators, receptor internalization, and navigating the transition from Modulators and Receptor Signaling Beyond the Membrane Opioid receptors belong to a class of GPCRs where The first allosteric modulators of opioid receptors were discovered through an academic-industry collaboration Scientific Themes of the Conversation Allosteric modulation of opioid receptors - mechanism, selectivity or endogenous opioids at the binding pocket, allosteric modulators act at a distinct site on the receptor

Graciela Piñeyro on what happened when her lab tested biased agonism at the μ-opioid receptor across 25 ligands, why δ-opioid receptors recycle from the lysosome, and the quantitative pharmacology that Across 25 ligands profiled at the μ-opioid receptor, the team found no bias, only partial agonism. Her lab now studies δ- and μ-opioid receptor signaling, biased agonism, receptor trafficking and recycling Long treated as a non-recycling receptor destined for degradation, the δ-opioid receptor can in fact

His work focuses on understanding how ligands interact with receptors such as the μ-opioid and κ-opioid Kim’s group interacts with multiple opioid receptors, acting as an antagonist at one receptor and an My favorite GPCR is not the opioid receptors. Instead, it’s the galanin receptor . Dr. Some studies also suggest that the galanin receptors may interact with the μ-opioid receptor. The second “aha moment” came when I solved the structures of the μ-opioid and κ-opioid receptors bound

Catherine Demery shares how she found clarity and purpose in academic opioid research. , receptors. investigates how fentanyl and xylazine shut down breathing through different mechanisms—work that blends receptor Listen now and see how one scientist is turning molecules into a mission, bridging the gap between receptor pharmacology and the urgent fight to save lives in the opioid epidemic.

Ph.D. from Department of Pharmacology, University of Washington (1992, mentor Charley Chavkin , sigma receptors Postdoc with Graeme Henderson (Bristol, opioids and Ca signaling) and Mac Christie (Sydney, opioids in Grant-funded independent research positions from 2001 at University of Sydney (opioids and sensory neurons visiting scientist with Ed McCleskey, sensory neuron properties); Pain Management Research Institute (more opioids Focus on study of drugs and toxins on GPCR (opioid, cannabinoid receptor) and ion channel (K, Ca, TRP

whether opioid receptors were even proteins, to the cryo-EM-driven structure-function loops that now His lab works on serotonin, dopamine, and opioid receptor structure, function, and drug discovery, with Roth's lab identified salvinorin A as a kappa opioid receptor agonist. reserve and capture coupling close to the receptor. 06:30 When the field debated whether opioid receptors were even proteins 11:31 The "dumb luck" of starting

Arun Shukla on how two beta-arrestin isoforms regulate over 800 receptors, why "non-canonical" GPCRs are nature's own biased receptors, and building a structural pharmacology lab in India. << Back to podcast Biased agonism is harder than the opioid story suggested The neat bifurcation between G-protein and beta-arrestin signaling that drove early opioid receptor drug design has not held up cleanly in subsequent studies tail was expected to be receptor-specific.

Slosky’s research is focused on understanding how neuropeptide G protein-coupled receptors (GPCRs) regulate motivated behavior and how these receptors can be targeted for therapeutic benefit. These ligands stimulate receptor β-arrestin recruitment without activating canonical G protein signaling Because BAMs engage less well-conserved allosteric sites and exert pathway-specific effects on receptor selectivity can be leveraged in the development of safe and effective treatments for stimulant and opioid

Neuroscience at the University of Ottawa as a Postdoctoral Fellow to explore novel G protein-coupled receptor at The Rockefeller University, where she study’s the signaling and degradation of G protein-coupled receptors lab where she helped to investigate the role of various ATP-sensitive potassium channels in pain and opioid to understand the mechanism by which a new class of biased allosteric modulators for the neurotensin receptor

With respect to GPCRs, I'm particularly interested in peptide/small protein receptors and the mechanisms With a special emphasis on G protein coupled receptors and receptor activity modifying proteins in vascular motivated behavior and how these receptors can be targeted for therapeutic benefit. Because BAMs engage less well-conserved allosteric sites and exert pathway-specific effects on receptor selectivity can be leveraged in the development of safe and effective treatments for stimulant and opioid

A combined in silico approach to design peptide ligands with increased receptor-subtype selectivity Adam A2B adenosine receptor-triggered intracellular calcium mobilization: Cell type-dependent involvement selectivity Ligand-Independent Spontaneous Activation of Purinergic P2Y6 Receptor Under Cell Culture Soft Substrate 🔎 GPCR KEYWORDS Class-A G protein-coupled receptors , Lophotrochozoa , echinoderms , nerve injury , neuropathic pain , spinal cord dorsal horn , OPN3 , cAMP signalin g , MC4R , docking , opioid

She has done extensive work on the molecular pharmacology of opioid receptors and is currently focusing

/PhD, a rejection letter pivoted him into a PhD program at the University of Iowa, where he studied opioid Driven by the opioid crisis and the lack of non-addictive pain treatments, Ajay co-founded Blue Therapeutics

Eleonora Comeo synthesizes fluorescent ligands to watch adenosine receptor pharmacology happen in living cells - and explains why targeting these receptors keeps failing. << Back to podcast list Strategic One reason is that selectivity in this family is not just a matter of receptor subtype. in another tissue, because the receptor is already doing something important there. transfected receptor signal from endogenous background.

, odorant receptors, and the trace amine-associated receptors that may one day treat depression. << Back Chemosensory receptors — bitter taste receptors (TAS2Rs), odorant receptors, and trace amine-associated Bitter taste receptors have been identified in the heart and intestine, olfactory receptors in the brain Her group now studies taste receptors, odorant receptors, and trace amine-associated receptors using olfactory system 19:03 Inside a computational workflow for orphan receptors 29:14 Bitter receptors in

Gunnar Schulte of Karolinska Institute makes the case that frizzled receptors are GPCRs — through G-protein The biggest question is how we don't understand how the ligand interacts with the receptor, how the receptor That is my strongest argument for the GPCR nature of these receptors." section Receptor Biology and Signaling at the Department of Physiology and Pharmacology. , the relevance of receptor dynamics, and receptor complex composition for signal initiation and specification

matchmaking - applying recommendation system logic to the bitter taste receptor family Sweet taste receptor receptor inhibitor suppresses the sweetness of heavy water. Taste receptor expression throughout the body reshapes the meaning of drug off-targets Bitter taste receptors properties of both - that can suggest candidate receptors for any new compound. - bitter taste receptors in the airways, gut, heart, and cancer tissues 19:37 - Sweet taste receptors

Pluznick explores what changes when olfactory receptors are treated not as smell receptors but as general-purpose Her lab studies the role of understudied GPCRs — olfactory receptors, taste receptors, and orphan GPRs Reframing olfactory receptors as chemosensors. The name "olfactory receptor" narrows the imagination. Dr. Mice have ~1,000 olfactory receptors; humans have ~350.

and chemokine receptor systems, including CCR2. Receptors in Complexes Behave Differently Than Receptors in Isolation Standard drug screens present a receptor as a discrete, isolated target. In the body, that receptor is complexing with other receptors, scaffold proteins, and cytoskeletal elements receptors are complexing.

Elva Zhao on biased agonism at the GLP-1 receptor, G protein regulation, and building a mechanistic picture podcast list Strategic Partner(s) Elva Zhao: G Protein Regulation and Biased Signaling at the GLP-1 Receptor The GLP-1 receptor is among the most clinically validated targets in metabolic disease - yet the signaling Her PhD at Western University focused not on receptors but on G protein cycle regulation - RGS proteins Nigel Bennett on biased signaling at the PAR2 receptor, then with Profs.

Nobel laureate Robert Lefkowitz traces the accidental origins of his receptor research — from a Vietnam receptors are discrete molecular entities. Receptors were an unproven concept when Lefkowitz chose to study them When Dr. existence of receptors. There's no such thing as a receptor.

Cheloha builds nanobody-GPCR ligand conjugates that rescue weak peptides, engineer receptor selectivity to podcast list Strategic Partner(s) Ross Cheloha: Nanobody-GPCR Conjugates and the Engineering of Receptor Selectivity The parathyroid hormone receptor sits at the intersection of calcium homeostasis, bone metabolism How does receptor conformation shape the duration of downstream signaling? And can selectivity for one receptor subtype be engineered without redesigning the ligand from scratch

From chemokine receptors at Rockefeller to founding Dr. GPCR during COVID — the career arc behind the ecosystem built for the field's unreached receptors. << multiple chemokines bind multiple receptors. The 250-receptor problem sits in plain sight. Without that tissue, GPCRs stay siloed by receptor family and by lab.

Terry Kenakin on detecting, quantifying, and applying receptor signaling bias in GPCR drug discovery. This phenomenon, receptor signaling bias or functional selectivity, is now recognized as a meaningful It is a consequence of ligand-dependent receptor conformations and allosteric probe dependence, and it The Biology Behind Bias Ligands produce differential pathway engagement at a single receptor because they stabilize distinct receptor conformations.