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purinergic receptors and, most recently, proton-sensing GPCRs in the tumor microenvironment. Biased signaling is real but harder to exploit than expected GPR68 couples to both Gq and Gs, and the And the answer was PAR1, the thrombin receptor. Alfred Gillman , co-recipient of the 1994 Nobel Prize in Physiology or Medicine for their discovery of G-proteins From that point on, Paul was hooked and has since studied receptor function in human physiology, receptor

Summary Arthur's Career Journey and Allosteric Receptors Yamina and Arthur discussed Arthur's career journey and his contributions to the field of pharmacology, with a focus on allosteric receptors and Allosteric Modulation and Drug Discovery Yamina and Arthur delved into the complexities of protein-protein They discussed various modulatory elements, such as RAMPs, G proteins, and GRKs, with Arthur recounting his initial collaboration with Patrick Sexton on RAMPs and amylin receptors.

The main focus of his lab’s research is on the mechanisms underlying biased agonism at chemokine receptors The chemokine system is relatively unique in having multiple receptors and multiple ligands that display His group and others have shown that many of these ligands act as biased agonists for the same receptor identifying novel signal transduction mechanisms of GPCRs, such as the formation of complexes between G proteins and beta-arrestins.

multiple areas of GPCR research such as sequence alignments, generic numbering systems, structure data, G protein and arrestin coupling and more.

multiple areas of GPCR research such as sequence alignments, generic numbering systems, structure data, G protein and arrestin coupling and more.

organization at Bristol-Myers Squibb, where he leads research spanning GPCR pharmacology, enzymology, and protein , which were among the first experimental demonstrations that a GPCR could signal through parallel G protein pathways in a ligand-dependent manner. conservation of biased receptor function across receptor classes The physiologist's approach to mechanistic The same logic applies to cytokine receptors, nuclear hormone receptors, and receptor tyrosine kinases

are expressed and studied as isolated proteins. His group developed BRET and NanoBRET-based live-cell platforms that capture protein-protein interactions In the body, that receptor is complexing with other receptors, scaffold proteins, and cytoskeletal elements receptors are complexing. They're interacting with the cytoskeleton, with other proteins, with other receptors, and that will change

Her team at InterAx models receptor signaling pathways as systems of time-dependent equations, then runs ten to fifteen pharmacological parameters — internalization rates, recycling and degradation rates, G protein affinity for the ligand-receptor complex, and more — rather than a single EC50 or a single bias The next challenge is multi-receptor, multi-disease complexity. The computational tools that now describe single receptors will need to extend to how multiple receptors

G. Aditya Kumar About Dr. G. Aditya Kumar Dr. at Hyderabad, India, where he studied the interaction of membrane cholesterol with the serotonin-1A receptor and its effects on receptor signaling and endocytosis. molecular pharmacology, subcellular trafficking, and membrane biology to better understand how the dynamic receptor G.

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

Johnson explains why the circuit matters more than the receptor. << Back to podcast list Strategic Partner coupled to Gi/o proteins, sits at a critical junction in this process. Kari Johnson's research follows this receptor from the bench to the behaving animal, using optogenetics That breadth is a signal of the receptor's centrality in CNS function. The question, in Johnson's framing, is not which receptor you prefer, but which receptor is correctly

Among other projects, I studied the role of β-arrestin in G protein trafficking, the impact of GPCR ubiquitination early tasks at Michelle’s lab, which involved creating stable cell lines and identifying potential protein the potential of multiplexing assays in expanding the scope of scientific exploration and finding new protein Yamina shared her experiences at Rockefeller, where she studied chemical receptors.

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

John Streicher: Reorganizing Opioid Signaling Beyond the Receptor The dominant strategy for improving opioid therapy has been to engineer new ligands at the receptor itself — biased agonists, partial agonists In the brain, HSP90 promotes ERK activation downstream of the mu opioid receptor and is required for Receptor signaling assays showed efficacy shifts in the spinal cord and tolerance attenuation in the HSP90 is 2–3% of the protein content of every eukaryotic cell.

Chemosensory receptors — bitter taste receptors (TAS2Rs), odorant receptors, and trace amine-associated For her, the work isn't abstract: she spent five months staring at empty protein crystals during her Her group now studies taste receptors, odorant receptors, and trace amine-associated receptors using Pizio spent five months crystallizing carbonic anhydrase 2 with small molecules and seeing only empty proteins "For five months, my protein was always empty at the X-ray.

The same library has produced antibodies against orphan GPCRs and receptors without peptide ligands, bivalent IgG, the team hands functional biology teams a molecule that is ready for flow cytometry and receptor Receptors within a family share sequence and surface topography, so an antibody recovered against one 09:17 Why antibodies to GPCRs have stayed so intractable 09:29 The motif-directed library — encoding receptor motifs into CDR3 12:34 Why one antibody can open up a whole receptor family 14:36 Eight to ten weeks

He describes the purification and cloning of the CGRP receptor, the identification of receptor activity-modifying proteins (RAMPs), and the realization that CGRP signaling required receptor complexes rather than a single seven-transmembrane protein, reshaping thinking about peptide receptor activation and ligand binding of peptide receptor activation and made clear that receptor complexes, not single proteins, could underlie Target Validation Is Harder Than Cloning a Receptor .

Livingston on allosteric opioid modulators, receptor internalization, and navigating the transition from internalization using live-cell imaging approaches that track receptor dynamics in real time. Internalized receptors don't stop working The membrane-centric view of receptor pharmacology assumes signaling ends when a receptor is endocytosed. Product Manager at Gator Bio , a biotechnology company providing solutions to researchers studying protein-protein

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

Where a receptor signals, how long it remains engaged, and which membrane it occupies all shape the downstream Coverage spans the mechanisms of receptor signaling and trafficking, labeling strategies and quantitative where he heads the Department of Metabolism and Systems Science and co-directs the Centre of Membrane Proteins and Receptors (COMPARE). His Masterclass brings this single-molecule, imaging-driven view of receptor signaling directly to Dr

Their pharmacological complexity is amplified by receptor activity modifying proteins (RAMPs), three single-pass membrane proteins that associate with these receptors to create pharmacologically distinct Hay examines the molecular pharmacology of the calcitonin receptor and calcitonin-like receptor - with and calcitonin-like receptor - and their interactions with RAMPs. - the canonical CGRP receptor in migraine.

Fellow, and Director of the Australian Research Council Centre for Cryo-electron Microscopy of Membrane Proteins in the study of GPCRs, biased agonism, and also on allosteric interactions between GPCRs and other proteins , a corresponding member of the International Union of Basic and Clinical Pharmacology Committee on Receptor

Yet much remains to be learned about how these 800-plus receptors are expressed and how they function Multipass transmembrane proteins are genuinely difficult targets. Part of the gap is the reagents. Identifying an immunoreactive antigen sequence that is specific for a single receptor and detectable He transitioned from clinical medicine to academic research at UC Irvine, where he worked on protein

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

. << Back to podcast list Strategic Partner(s) Scaling GLP 1 Receptor Tools Through Academia Industry access aren’t planned from the start Why fluorescence-based assays outperform antibodies for studying receptor focuses on bottom-up chemical tool development for imaging and interrogating GPCRs and other cell-surface proteins His research focuses on class B GPCRs, including the GLP-1 and GIP receptors, with an emphasis on understanding how these receptors operate within complex tissues such as the pancreas and brain.

.” — Alex Serafini Blind Spots: The Underestimated Role of RGS Proteins in Pain Although not a self-proclaimed specialist, Serafini found himself repeatedly drawn to them, or more precisely, to RGS (Regulators of G protein Signaling) proteins. and addiction/withdrawal on the mesocorticolimbic system, focusing on transcription factor and RGS protein maladaptations, behavioral RGS protein drug "screening", and the role of SARS-CoV-2 on CNS function

and received my Ph.D. in Molecular Medicine in 2010 after studying the orphan atypical cannabinoid receptor I was fascinated by the multitude of processes that are regulated/dysregulated by GPCRs and RGS proteins A fungal serine protease allergen with GPCR-modulating features was discovered as a new biomarker and I studied the function of RGS5, calcium-sensing receptor, and an orphan adhesion GPCR, GPR64/ADGRG2 in

the early days of ion channel chemistry to pioneering peptide–fluorophore conjugates for the GLP-1 receptor Why targeting the pharmacologically relevant surface-exposed receptor pool changes the way scientists The moment when super-resolution imaging revealed nanoscale receptor domains that conventional tools Berlin, focusing on developing fluorescent chemical tools to visualize GPCRs and other cell-surface proteins lab integrates synthetic chemistry, theoretical chemistry, cell biology, and imaging to understand receptor

Research interests: Signaling mechanisms involving GPCRs and heterotrimeric G proteins" Dr.

designed to assess the kinetics of unlabelled compounds (and chemical fragments) and the use of purified receptor / effector proteins as tools for drug discovery. " Dr.