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PXD041346

PXD041346 is an original dataset announced via ProteomeXchange.

Dataset Summary
TitleCellular Validation of Chemically Improved Inhibitor Identifies Monoubiquitination on OTUB2
DescriptionUbiquitin thioesterase OTUB2, a cysteine protease from the ovarian tumor (OTU) deubiquitinase superfamily, is associated with enhanced expression during tumor progression and metastasis. Development of OTUB2 inhibitors is therefore believed to be therapeutically important, yet potent and selective small-molecule inhibitors targeting OTUB2 are scarce. Here, we describe the development of an improved OTUB2 inhibitor, LN5P45, comprising a chloroacethydrazide moiety that covalently reacts to the active-site cysteine residue. When added to cells, LN5P45 shows outstanding target engagement and proteome-wide selectivity. Importantly, we found that LN5P45 and the other OTUB2 inhibitors strongly induce monoubiquitination of OTUB2 via lysine 31. Thus, our findings provide novel insights for the design of future OTUB2-related therapeutics and open new questions regarding the understanding of OTUB2 regulation at the post-translational modification level.
HostingRepositoryPRIDE
AnnounceDate2023-06-27
AnnouncementXMLSubmission_2023-06-27_03:49:49.631.xml
DigitalObjectIdentifier
ReviewLevelPeer-reviewed dataset
DatasetOriginOriginal dataset
RepositorySupportUnsupported dataset by repository
PrimarySubmitterRaymanTjokrodirijo
SpeciesList scientific name: Homo sapiens (Human); NCBI TaxID: 9606;
ModificationListubiquitinylated lysine
InstrumentOrbitrap Fusion Lumos; Orbitrap Exploris 480
Dataset History
RevisionDatetimeStatusChangeLog Entry
02023-04-05 03:52:30ID requested
12023-06-27 03:49:50announced
Publication List
Dataset with its publication pending
Keyword List
submitter keyword: OTUB2, small-molecule inhibitor, monoubiquitination
Contact List
Peter A. vanVeelen
contact affiliationHead Proteomics Group Leiden University Medical Center, Center for Proteomics and Metabolomics, PO Box 9600, Postal zone P1-Q, 2300 RC Leiden, The Netherlands
contact emailP.A.van_Veelen@lumc.nl
lab head
RaymanTjokrodirijo
contact affiliationLeiden University Medical Center, Proteomics group
contact emailR.T.N.Tjokrodirijo@lumc.nl
dataset submitter
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Dataset FTP location
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