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Record W3083832329 · doi:10.1021/jacs.0c05587

Development of High-Specificity Fluorescent Probes to Enable Cannabinoid Type 2 Receptor Studies in Living Cells

2020· article· en· W3083832329 on OpenAlexfundno aff
Roman C. Sarott, Matthias V. Westphal, Patrick Pfaff, Claudia Korn, David A. Sykes, Thais Gazzi, Benjamin Brennecke, Kenneth Atz, Marie Weise, Yelena Mostinski, Pattarin Hompluem, Eline J. Koers, Tamara Miljuš, Nicolas J. Roth, Hermon Asmelash, Man Vong, Jacopo Piovesan, Wolfgang Guba, Arne C. Rufer, Eric A. Kusznir, Sylwia Huber, Catarina Raposo, Elisabeth A. Zirwes, Anja Osterwald, Anto Pavlovic, Svenja Moes, Jennifer Beck, Irene Benito‐Cuesta, María T. Grande, Samuel Ruiz de Martı́n Esteban, Alexei Yeliseev, Faye Drawnel, Gabriella Widmer, Daniela Holzer, Tom van der Wel, Harpreet Mandhair, Cheng-Yin Yuan, William R. Drobyski, Yurii Saroz, Natasha L. Grimsey, Michael Honer, Jürgen Fingerle, Klaus Gawrisch, Julián Romero, Cecilia J. Hillard, Zoltán V. Varga, Mario van der Stelt, Pál Pacher, Jürg Gertsch, Peter J. McCormick, Christoph Ullmer, Sergio Oddi, Mauro Maccarrone, Dmitry B. Veprintsev, Marc Nazaré, Uwe Grether, Erick M. Carreira

Bibliographic record

VenueJournal of the American Chemical Society · 2020
Typearticle
Languageen
FieldMedicine
TopicCannabis and Cannabinoid Research
Canadian institutionsnot available
FundersNational Heart, Lung, and Blood InstituteLeibniz-GemeinschaftMedical Research CouncilMinistero dell’Istruzione, dell’Università e della RicercaEidgenössische Technische Hochschule ZürichRocheCanada Excellence Research Chairs, Government of CanadaSchweizerischer Nationalfonds zur Förderung der Wissenschaftlichen ForschungUniversity of BernF. Hoffmann-La RocheUniversità degli Studi dell'AquilaNational Science FoundationQueen Mary University of LondonMinisterio de Economía y Competitividad
KeywordsChemistryFlow cytometryReceptorCannabinoid receptorConfocal microscopyCell typeCell biologyEndocannabinoid systemCellCannabinoidG protein-coupled receptorBiochemistryMolecular biologyBiology

Abstract

fetched live from OpenAlex

Abstract Pharmacological modulation of cannabinoid type 2 receptor (CB2R) holds promise for the treatment of numerous conditions, including inflammatory diseases, autoimmune dis­orders, pain, and cancer. Despite the significance of this receptor, researchers lack reliable tools to address questions concerning the expression and complex mechanism of CB2R signaling, especially in cell-type and tissue-dependent contexts. Herein, we report for the first time a versatile ligand platform for the modular design of a collection of highly specific CB2R fluorescent probes, used successfully across applications, species, and cell types. These include flow cytometry of endogenously expressing cells, real-time confocal microscopy of mouse splenocytes and human macrophages, as well as FRET-based kinetic and equilibrium binding assays. High CB2R specificity was demonstrated by competition experiments in living cells expressing CB2R at native levels. The probes were effectively applied to FACS analysis of microglial cells derived from a mouse model relevant to Alzheimer’s disease.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame machine prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. The Gemma side is a direct model label for every work in the frame, read from the title-only record. The Codex side is a classifier learned from the 10,348 direct Codex labels and calibrated to design-weighted sample rates; fields without enough sample support carry no Codex call. Candidate is the union of the two sides; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels.

metaresearch head score (Codex)0.001
metaresearch head score (Gemma)0.001
Version: metacan-v3-hybrid-931329e0061cValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: Bench or experimental
GenreCandidate signal: Empirical · Consensus signal: none
Teacher disagreement score0.002
Threshold uncertainty score0.006

Distilled classifier scores by category (both heads)

CategoryCodexGemma
Metaresearch0.0010.001
Meta-epidemiology (narrow)0.0010.000
Meta-epidemiology (broad)0.0010.000
Bibliometrics0.0000.000
Science and technology studies0.0000.000
Scholarly communication0.0010.001
Open science0.0010.001
Research integrity0.0010.001
Insufficient payload (model declined to judge)0.0020.001

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.039
GPT teacher head0.311
Teacher spread0.273 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one source (direct Gemma or distilled Codex), not a consensus.

The models applied no category: nothing in the taxonomy fit this work.
Study designBench or experimental
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations49
Published2020
Admission routes1
Has abstractyes

Explore more

Same venueJournal of the American Chemical SocietySame topicCannabis and Cannabinoid ResearchFrench-language works237,207