PXD008460 is an
original dataset announced via ProteomeXchange.
Dataset Summary
Title | A selective photoaffinity probe enables assessment of cannabinoid CB2 receptor expression and ligand engagement in human cells |
Description | Chemical 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. |
HostingRepository | PRIDE |
AnnounceDate | 2024-10-22 |
AnnouncementXML | Submission_2024-10-22_04:37:35.451.xml |
DigitalObjectIdentifier | |
ReviewLevel | Peer-reviewed dataset |
DatasetOrigin | Original dataset |
RepositorySupport | Unsupported dataset by repository |
PrimarySubmitter | Bogdan Florea |
SpeciesList | scientific name: Cricetulus griseus (Chinese hamster) (Cricetulus barabensis griseus); NCBI TaxID: 10029; scientific name: Homo sapiens (Human); NCBI TaxID: 9606; |
ModificationList | monohydroxylated residue; iodoacetamide derivatized residue |
Instrument | Synapt MS; LTQ Orbitrap |
Dataset History
Revision | Datetime | Status | ChangeLog Entry |
0 | 2017-12-15 00:53:33 | ID requested | |
1 | 2018-06-15 05:32:32 | announced | |
2 | 2019-02-26 08:05:59 | announced | Updated publication reference for PubMed record(s): 29420021. |
⏵ 3 | 2024-10-22 04:37:43 | announced | 2024-10-22: 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 affiliation | Molecular Physiology, Leiden Institute for Chemistry, Leiden University, The Netherlands |
contact email | m.van.der.stelt@chem.leidenuniv.nl |
lab head | |
Bogdan Florea |
contact affiliation | Leiden Institute for Chemistry |
contact email | b.florea@chem.leidenuniv.nl |
dataset submitter | |
Full Dataset Link List
Dataset FTP location
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PRIDE project URI |
Repository Record List
[ + ]
[ - ]
- PRIDE
- PXD008460
- Label: PRIDE project
- Name: A selective photoaffinity probe enables assessment of cannabinoid CB2 receptor expression and ligand engagement in human cells