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PXD008460

PXD008460 is an original dataset announced via ProteomeXchange.

Dataset Summary
TitleA selective photoaffinity probe enables assessment of cannabinoid CB2 receptor expression and ligand engagement in human cells
DescriptionChemical tools and methods that report on G protein-coupled receptor (GPCR) expression levels and receptor occupancy by small molecules are highly desirable. We report the development of LEI121 as a photoreactive probe to study the type 2 cannabinoid receptor (CB2R), a promising GPCR to treat tissue injury and inflammatory diseases. LEI121 is the first CB2R-selective bifunctional probe that covalently captures CB2R upon photoactivation. An incorporated alkyne serves as ligation handle for the introduction of reporter groups. LEI121 enables target engagement studies and visualization of endogenously expressed CB2R in HL-60 as well as primary human immune cells using flow cytometry. Our findings show that strategically functionalized probes allow monitoring of endogenous GPCR expression and engagement in human cells using tandem photo-click chemistry and hold promise as biomarkers in translational drug discovery.
HostingRepositoryPRIDE
AnnounceDate2024-10-22
AnnouncementXMLSubmission_2024-10-22_04:37:35.451.xml
DigitalObjectIdentifier
ReviewLevelPeer-reviewed dataset
DatasetOriginOriginal dataset
RepositorySupportUnsupported dataset by repository
PrimarySubmitterBogdan Florea
SpeciesList scientific name: Cricetulus griseus (Chinese hamster) (Cricetulus barabensis griseus); NCBI TaxID: 10029; scientific name: Homo sapiens (Human); NCBI TaxID: 9606;
ModificationListmonohydroxylated residue; iodoacetamide derivatized residue
InstrumentSynapt MS; LTQ Orbitrap
Dataset History
RevisionDatetimeStatusChangeLog Entry
02017-12-15 00:53:33ID requested
12018-06-15 05:32:32announced
22019-02-26 08:05:59announcedUpdated publication reference for PubMed record(s): 29420021.
32024-10-22 04:37:43announced2024-10-22: Updated project metadata.
Publication List
10.1021/jacs.7b11281;
Soethoudt M, Stolze SC, Westphal MV, van Stralen L, Martella A, van Rooden EJ, Guba W, Varga ZV, Deng H, van Kasteren SI, Grether U, IJzerman AP, Pacher P, Carreira EM, Overkleeft HS, Ioan-Facsinay A, Heitman LH, van der Stelt M, Receptor Expression and Ligand Engagement in Human Cells. J Am Chem Soc, 140(19):6067-6075(2018) [pubmed]
Keyword List
curator keyword: Biological
submitter keyword: target engagement, CB2 receptor,GPCRs, photo-affinity labeling, bio-orthogonal chemistry
Contact List
Mario van der Stelt
contact affiliationMolecular Physiology, Leiden Institute for Chemistry, Leiden University, The Netherlands
contact emailm.van.der.stelt@chem.leidenuniv.nl
lab head
Bogdan Florea
contact affiliationLeiden Institute for Chemistry
contact emailb.florea@chem.leidenuniv.nl
dataset submitter
Full Dataset Link List
Dataset FTP location
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PRIDE project URI
Repository Record List
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