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Bitter taste receptors (TAS2Rs) are a poorly understood subgroup of G protein-coupled receptors (GPCRs). The experimental structure of these receptors has yet to be determined, and key-residues controlling their function remain mostly unknown. We designed an integrative approach to improve comparative modeling of TAS2Rs. Using current knowledge on class A GPCRs and existing experimental data in the literature as constraints, we pinpointed conserved motifs to entirely re-align the amino-acid sequences of TAS2Rs. We constructed accurate homology models of human TAS2Rs. As a test case, we examined the accuracy of the TAS2R16 model with site-directed mutagenesis and in vitro functional assays. This combination of in silico and in vitro results clarifies sequence-function relationships and proposes functional molecular switches that encode agonist sensing and downstream signaling mechanisms within mammalian TAS2Rs sequences. Read full article

Bioanalysis   2018 , 10  (19), 1609–1623. https://doi.org/10.4155/bio-2018-0150 . (11)      Showalter Bioconjugate Chem. 2013 , 24  (11), 1907–1916. https://doi.org/10.1021/bc400328m . (16)      Morrison Analytical Biochemistry   1988 , 174  (1), 101–120. https://doi.org/10.1016/0003-2697(88)90524-6 . (17 Principles and Biophysical Applications of Lanthanide-Based Probes. Nature Biotechnology   2003 , 21  (1), 86–89. https://doi.org/10.1038/nbt765 . (24)      Zwier, J.

. 👉 In biotech, where cycles are long and feedback is slow, this gap becomes even more pronounced. Biotech teams operate across disciplines, timelines, and incentives. Attila runs focused strategy consultations for biotech founders who are ready to lead with clarity, not

Sneak Peak:  Human Substance P–NK1R interactions observed by NMR; Endocrine Metabolic GPCRs 2026 and Biophysical In Episode 3 of 3  of our series with Celtarys Research , leaders from academia and biotech unpack what

Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves Kenakin stresses, the apparent simplicity collapses once biological reality intrudes. Take home message: interpret orthosteric binding data only after verifying that the biology behaved as Complex Two-Stage Biology Behind Orthosteric Binding GPCR pharmacology rarely follows the neat Langmuir Clues that point to true multiple-site binding rather than two-stage GPCR biology: Disrupting G protein

Most GPCR programs don’t fail because of weak molecules—they fail because biology behaves differently Principal Scientist—GPCR Pharmacology; Principal Scientist—In Vitro Pharmacology; Research Associate—Biologics Translate potency and efficacy realistically  → Recognize when deviations reflect biology rather than why chemical design can outperform antibodies and how rigorous assay validation bridges chemistry and biology GPCR Premium Membership Gives You an Edge Premium gives GPCR scientists and biotech teams a single, trusted

as the underlying system allowed—amplified, buffered, redirected, or reshaped by layers of receptor biology This isn’t experimental noise—it’s biology. Biology rarely gives one. It equips pharmacologists, discovery teams, and biotech leaders to see around mechanistic corners, recognize

His career moved through veterinary school, immunology, neuroendocrinology, and finally into islet biology receptors behave in intact tissue, Hodson needed people who saw problems differently — chemists, structural biologists This collaboration reshaped the way Hodson’s lab studies receptor biology. will hinge on the teams who can map GPCR signaling with precision and design therapies that fit real biology They’re team problems — the kind that require chemistry, physiology, pharmacology, structural biology

kinetics, and ligand interactions in intact cells offers advantages that extend far beyond traditional biochemical These challenges can obscure real biological signals and complicate the identification of robust hits Unlike biochemical assays, which reduce biology to a single readout, HCS captures whole-cell phenotypes Assay Design and Pilot Optimization Successful HCS begins with a clearly defined biological question Imaging Calibration and Acquisition These steps ensure that quantitative signals reflect biology, not

This solved a long-standing problem in GPCR biology: You can't understand signaling if you can’t see 

have now been shared with hundreds of labs , accelerating research in obesity, hypertension, platelet biology Why it matters: Personalizing care depends on understanding biological variability.

Yet, any pharmacologist who’s pushed beyond textbook theory knows: biology rarely plays fair. Schild analysis remains the simplest, most revealing conversation we can have with biology.

Career opportunities:  GPCR Biology; Protein Science. GPCR Podcast: Visualizing GLP-1 & GIP Receptors in Islets and Brain Understanding incretin biology depends GPCR scientists, translational pharmacologists, biotech discovery teams, and decision-makers who need

GPCR Foundry  — our R&D and biotech hub designed to bridge GPCR science with execution. The Dr. GPCR Foundry: Science Meets Execution The Foundry is where we bring together biotech innovators, Venture , he shares decades of expertise in an accessible, on-demand format for scientists across academia, biotech

Today, Carlsson is Professor of Computational Biochemistry at Uppsala University and one of the strongest For receptor assays and the biological interpretation of ligands, he relies on a network of collaborators Beyond Academia: Advising Biotech Carlsson’s collaborative philosophy has also found a place in the biotech The GPCR Challenge What makes collaboration non-negotiable in GPCR research is the biology itself. Structural biologists may capture snapshots of receptor conformations, but lack large-scale screening

Yet even with the structural biology revolution, one stubborn hurdle persists: prediction.   Jens Carlsson , Professor of Computational Biochemistry at Uppsala University. Translational Impact for Drug Discovery While the Carlsson lab is rooted in academia, its impact extends into biotech Modeling That Moves the Field Forward The Carlsson lab exemplifies how c omputational biochemistry can

Nicholas Kapolka , Geoffrey Taghon , and Daniel Isom  for their research on Advances in yeast synthetic biology for human GPCR biology and pharmacology Dr. from October 23-25, 2024, to connect with fellow scientists and explore the latest in adhesion GPCR biology protein-coupled receptor (GPCR) gene variants and human genetic disease Advances in yeast synthetic biology for human G protein-coupled receptor biology and pharmacology Industry News Muscarinic drugs breathe

Today, Carlsson is a Professor of Computational Biochemistry at Uppsala University and one of the most When he moved to Uppsala in the late 1990s to study engineering, it was biotechnology—then on the rise—that through a practical suggestion: explore a new protein family that was gaining traction in the structural biology Collaborating with chemists, biologists, and pharmacologists not only made his predictions more useful

Breakthroughs this week:  nanomedicines targeting PAR2 for sustained analgesia; Emerging Voices in GPCR Biology Kenakin Trusted insights from biotech, pharma, and academia 🎬 Plus New: Lesson Trailers   Curious about GPCR scientists, translational pharmacologists, biotech discovery teams, and decision-makers who need

become brighter and have a longer lifespan as internalized receptors enter acidic endosomes—translating biology The biological validation came from Jean-Philippe Pin’s group at the Genomic Functional Institute in “You start wide with chemistry, you narrow with biology, and at the end—if you did it right—you open

October 23-25, 2024 Engage with your peers and delve into the latest developments in adhesion GPCR biology for its First-in-class GPR68 Inhibitor Asengeprast (FT011) AlphaProteo generates novel proteins for biology Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and Horizons 2024 September 30 - October 3, 2024 | 22nd Discovery on Target October 2024 | Biologics US /Structural Biologist Senior Scientist/Staff Scientist, Computational Chemistry Postdoc in GPCR mechanosensing

Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology GPCR Jobs Scientist I Cell Biology Pharmacology - The Hauser Group Postdoctoral Scholar – iPSC in cardiac and endothelial cell function Protein Biochemist /Structural Biologist Senior Scientist/Staff Scientist, Computational Chemistry Postdoc in GPCR mechanosensing behaviors in Sapap3 knockout mice Orphan GPCRs in Neurodegenerative Disorders: Integrating Structural Biology

When a compound’s off-rate is slower than its clearance, its biological effect outlives its plasma presence Dosing regimens aligned with biology, not just exposure. Kenakin Content trusted by biotech, pharma, and academia 💎 $2999/year — one conference cost = a full

Their global resource is now helping labs decode GPCR biology at scale. eyJ1IjoiaHR0cHM6Ly9kb2kub3JnLzEwLjExMTEvYnBoLjcwMDcyIiwiciI6ImUyZGZlOTFjLTM5YzgtNDA5Yi04NTUyLWI5NjUwNGRlNzc4MyIsIm0iOiJtYWlsX2xwIiwiYyI6IjAwMDAwMDAwLTAwMDAtMDAwMC0wMDAwLTAwMDAwMDAwMDAwMCJ9 The B2D consortium revives biodiversity Dive into this week’s research, tools, and biotech updates all in one place.

Explore this week’s research, tools, and biotech insights in one place. The insights are ready.

In this podcast, he lays out the mindset that helped shape products used across biotech and academia—and chemist David Parker on the probe chemistry, and with Jean-Philippe Pin’s team in Montpellier to validate biological teaming, testing, and failing smarter. 🚀 Why This Matters: Whether you’re launching a tool, starting a biotech

If you want your molecules to survive first contact with biology, enzyme inhibition must be part of your This week —NIH’s new GPCR biosensor push, a leadership shift at Septerna, and a bold thesis on stabilizing Kenakin Trusted insights across biotech, pharma, and academia 💎 $2,999/year — one conference cost = If you care about compartmentalized signaling and native-state biology, this is a sharp, readable tour Biosensors make once-invisible dynamics assayable at scale. Read the roundup ➤ Why Dr.

Understanding activation dynamics gives discovery teams a new design frontier: instead of blocking biology Kenakin Content trusted by biotech, pharma, and academia 💎 $2999/year — one conference cost = a full

curriculum with your topic suggestions Weekly new releases  to stay ahead of the science Content built for biotech how a series of bold pivots—from Cisbio’s HTRF platform to IP-One and now pHSense—reshaped how GPCR biology

If you’re in GPCR discovery or biotech R&D, this is a masterclass in turning deep science into scalable Initially applied to biomarkers in blood, its no-wash, miniaturized design caught the attention of high-throughput It started not with biology—but with chemistry. Revvity and academic collaborator Prof. It’s a strategic tool for decoding GPCR behavior in drug discovery and systems biology.