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system to meet that need: Dual-epitope tagged constructs (N-term FLAG, C-term 1D4) Compatible with multiple readouts: proximity, immuno assays, pulldowns Validated antibodies + digital search platform Entire “The students of today want biosensors, miniaturization, and multiplexing. ________________ Keyword Cloud : GPCR scientist network , GPCR online course , GPCR data platform , multiplex assays , GPCR drug discovery

The Tools to Detect Them Using the multiplexed GPCR library and Luminex assay , researchers can now: Sakmar and Kotliar’s system is multiplexed and scalable , able to test hundreds of interactions from GPCR ecosystem , multiplex assays

early curiosity around Family B GPCRs  set a 30-year trajectory in motion, culminating in a scalable, multiplexed With the help of Luminex technology and collaborators at SciLifeLab in Sweden , the lab built a multiplex assay  to study dozens of interactions simultaneously. “The beauty of multiplexing is that you can do many things with one pot of samples.” — Tom Sakmar Enter

From dual-epitope tagging to scalable multiplex assays, this conversation dives deep into the tools now

Thus we propose the use of fluorescent probes in GPCR screening assays due to their numerous advantages The advantages of Fluorescent Probes in GPCR assays over other methods Fluorescent ligands are made by receptors, tracking of their internalization and are also safer alternatives to radioligand binding assays The traditional binding assays for GPCRs use radioligands, whose limitations, especially safety concerns common starting point for employing fluorescent probes in GPCR assays.

Radioligands have been used to study GPCRs for decades, but with the advances in the fluorescence field, assays They are ligands labeled with radioactive isotopes which can be used in binding assays to quantify other Fluorescent Probes: Differences in Binding Assays Fluorescent ligands are a type of fluorescent probes that offer an alternative to radioligands in binding assays. GPCR-radioligand binding assays.

Imagine running a calcium assay and discovering your compound shows only weak activity. Kenakin dives deep into a widely used, often misunderstood tool in early drug discovery: the calcium assay Revered for its convenience, the FLIPR assay provides rapid insights into receptor activity. with strategic clarity. 📍 Foundational Level | Calcium Assays 📚 Part of Terry Kenakin’s Pharmacology Unlock "Calcium Assays" now

Enhance your GPCR research with deeper assay insights for more effective results. Terry's Corner – Assay Volume Control in GPCR Drug Discovery This week in Terry’s Corner, you’ll learn But behind every “new” assay is a decade of design, failure, and rethinking.

But what if the assay system itself  could be leveraged as a powerful experimental variable? Assay volume control does just that. The real question: are you letting your assay system dictate the wrong story? Clarify whether observed effects reflect true pharmacology or assay artifacts . Unlock Assay Volume Control Only in Terry’s Corner 🎬 Watch Course Trailers Not sure yet?

This technology enhances sensitivity and assay specificity . It can also be combined with  multiplexing . Saturation assays using CELT-335. A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery. A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery.

is to obtain a fluorescent ligand suitable for the Tag-lite® binding assays. (Ki) and saturation Tag-lite® binding assay (Kd).   1  Competition radioligand binding assay.  2  Saturation assay by Tag-lite® binding assay.  3  Displacement of specific [3H]-CP55940 binding in human HEK-CB1 assay and Kd= 42nM in Tag-lite®). Saturation assays using CELT-335.

August 2022 In vitro assays for the functional characterization of (psychedelic) substances at the serotonin More specifically, this review covers assays to monitor the canonical G protein signaling pathway (e.g measuring G protein recruitment/activation, inositol phosphate accumulation, or Ca2+ mobilization), assays recruitment or signaling, and assays to monitor receptor conformational changes. mechanism and linked to its specific execution, as these may heavily impact the assay outcome."

Thus, developing assays for commercially available probes such as CELT-419 would facilitate research assays, the radioligand binding method was used.  The estimated Z’ of the assay is 0.71, which is sufficient for HTS standards. Figure 3.   provide more information and alternatives for binding assays. multiple labels in a single study.

Eric Trinquet, a veteran innovator behind functional GPCR assays like HTRF and IP-One, believes rigid But those failures are where new paths emerge, often leading to transformative tools like the IP1 assay Eric Trinquet Built to Fail, Built to Win: Inside the IP1 Assay Origin Story The IP-One assay didn’t Instead, they focused on equilibrium-based assays and zeroed in on IP1 accumulation—pioneering a clean “We did a full dose-response and saw antagonism—all in one plate-based assay.

Every GPCR assay that makes it to market carries years of failures, late-night ideas, risky bets, and Functional assays for GPCRs—especially Gq-coupled receptors—were notoriously messy. Calcium flux? Trinquet’s team asked a bolder question: could they design equilibrium-based assays for pathways no one Built to Fail, Built to Win: The IP One Gamble After the success of their cAMP assay, Trinquet’s team Months were spent debating assay design. IP1 isn’t naturally abundant or easy to detect.

kinetics ✅ A framework to classify antagonists and rank compounds by offset rate, using rapid calcium assays The Hemi-Equilibrium Problem Calcium assays look simple. Flip it around, and you’ve got a shortcut: use depression of max in calcium assays to rapidly rank offset The reality is dynamic—ligands arrive, depart, and interact in ways that standard assays often miss. suggestions Practical insights  distilled from decades of pharmacology experience Whether you’re validating assays

Does Your Assay Agree With the Literature? Your experiment gives a pKB of 8.0. Is that consistent, or is your assay biased? to: Confirm whether your mean truly overlaps with accepted values Verify if binding and functional assays interchangeable with existing ones Instead of vague comparisons, you’ll have statistical clarity on whether your assay suggestions Practical insights  distilled from decades of pharmacology experience Whether you’re validating assays

developed and validated a label-free, liquid chromatography-mass spectrometry (LC-MS) based cell binding assay This assay was applied to various target classes, with particular emphasis on those for which protein-based binding assay can be difficult to achieve. In another example, this assay was applied to an ion channel target with its agonists, of which the determined binding affinity was consistent with functional assays.

Watch Episode 176 The first time Michelle ran a cyclic AMP assay, she did it with a single-channel pipette Assay samples were layered on trays of ice. These weren’t quaint inconveniences. We were doing assays on ice, pipetting one sample at a time. Those early cyclic AMP assays weren’t just cold and slow — they were part of a bigger puzzle. Mini Timeline: Manual assay years — technical rigor as foundation Technology boom — scaling curiosity

August 2022 Luciferase-based GloSensor™ cAMP assay: Temperature optimization and application to cell-based The GloSensor™ cAMP assay enables real-time monitoring of signaling downstream of many GPCRs. However, it is crucial to optimize assay conditions such as temperature. Here, we describe the temperature sensitivity and reversibility of the GloSensor™ cAMP assay, and which Nevertheless, the GloSensor™ cAMP assay can be applied to analyze signaling by a wide range of GPCRs

. • Assay Development Gets Real : Fluorescent tools and real-world biology don’t always match. Whether you’re designing the next assay, scouting a new therapeutic angle, or exploring career pivots

GPCR – Precision Tools for GPCR Assays Dr. GPCR and Celtarys Research have teamed up. Explore the partnership Multiplexing GPCR Discovery - Sakmar Lab’s Toolkit Goes Public The latest podcast features a discussion about a scalable GPCR-RAMP assay. Tom Sakmar, Emily Lorenzen, and Ilana Kotliar about creating a multiplex system with DUET-tagged constructs

October 2022 "We describe production of the human A2A adenosine receptor (A2AAR), a class A G protein-coupled receptor (GPCR) for 19F-NMR and single-molecule fluorescence (SMF) spectroscopy. We explain in detail steps shared between the two sample preparation strategies, including expression and isolation of A2AAR and assembly of A2AAR in lipid nanodiscs and procedures for incorporation of either 19F-NMR or fluorescence probes. Protocols for SMF experiments include sample setup, data acquisition, data processing, and error analysis. For complete details on the use and execution of this protocol, please refer to Wei et al. (2022) and Sušac et al. (2018)." Read more at the source #DrGPCR #GPCR #IndustryNews

GPCR gene variants and human genetic disease Ilana Kotliar , Thomas Sakmar , et al. for their study on Multiplexed Elements of a comprehensive and effective GPCR discovery Master advanced applications: Using new cellular assays 4th, 2024 GPCR Activation and Signaling ONE-GO: Direct detection of context-dependent GPCR activity Multiplexed codon-optimized clytin II gene in Chinese hamster ovary-K1 cells and its use in the G-protein-coupled receptor assays GPCR Events, Meetings, and Webinars September 18, 2024 | FREE Webinar - The value of GPCR cell-based assays

These limitations can impact data quality, reproducibility, and assay flexibility. Tag brightness and stability:  the brighter and more stable the better the assay outcome. 2.       Autofluorescence and multiplexing: Using far-red or near-infrared fluorophores can reduce background and support multi-parametric assays. 4.       CELT-240 in flow cytometry binding assays is suitable to measure the affinity of compounds for the D2

This analysis utilized a semi-quantitative multiplex PCR method, which allowed for the detection of both current study found that 133 of these receptors were also detected, highlighting the robustness of the assay previous study not detected in the current analysis, suggesting that variations in cell preparation and assay

chemokine/chemokine receptor axes in trafficking and oriented locomotion of mesenchymal stem cells in multiple sclerosis patients Multiple sclerosis (MS) is a specific type of chronic immune-mediated disease in

This Week’s GPCR Intelligence: From Set-Point Pharmacology to No-Wash Internalization Assays This week – Designing Drugs That Anticipate Physiological Pushback Most GPCR programs don’t fail because the assay specificity blocks promiscuous ligand confusion Lanthanide donors + d2 acceptors = high SNR, low background Multiplex-compatible

Methods & Updates in GPCR Research Multiplexed selectivity screening of anti-GPCR antibodies. FREE Symposium - IPI Surfacing (June 15, 2023) Training School on “Cell-based assays to study Adhesion - Antibody Engineering Scientist—Immuno-Oncology Convergent Research - Senior Scientist, Cell-Based Assay

September 2022 "Parkinson’s disease (PD) as a progressive neurodegenerative disorder arises from multiple Using multiplexed single-cell transcriptomics, we analyze human neural precursor cells (hNPCs) from sporadic