PXD008460

PXD008460 is an original dataset announced via ProteomeXchange.

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

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.

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]

curator keyword: Biological

submitter keyword: target engagement, CB2 receptor,GPCRs, photo-affinity labeling, bio-orthogonal chemistry

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

Dataset FTP location NOTE: Most web browsers have now discontinued native support for FTP access within the browser window. But you can usually install another FTP app (we recommend FileZilla) and configure your browser to launch the external application when you click on this FTP link. Or otherwise, launch an app that supports FTP (like FileZilla) and use this address: ftp://ftp.pride.ebi.ac.uk/pride/data/archive/2018/06/PXD008460

PRIDE project URI

• PRIDE
  1. PXD008460
     1. Label: PRIDE project
     2. Name: A selective photoaffinity probe enables assessment of cannabinoid CB2 receptor expression and ligand engagement in human cells