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PXD032284-2

PXD032284 is an original dataset announced via ProteomeXchange.

Dataset Summary
TitleKinobead profiling of PITCOINs1-3
DescriptionPhosphatidylinositol 3-kinase type 2a (PI3KC2a) and related class II PI 3-kinase isoforms are of rising biomedical interest because of their crucial roles in endocytic membrane dynamics, cell division and signalling, angiogenesis, and platelet morphology and function. Herein we report the development and characterization of PITCOINs, potent and highly selective small molecule inhibitors of PI3KC2 catalytic activity. PITCOIN compounds exhibit strong selectivity towards PI3KC2 due to their unique mode of interaction with the ATP binding site of the enzyme. We demonstrate that acute inhibition of PI3KC2-mediated synthesis of phosphatidylinositol 3-phosphates by PITCOINs impairs endocytic membrane dynamics and membrane remodelling during platelet-dependent thrombus formation. To our knowledge PITCOINs are the first potent and selective cell permeable inhibitors of PI3KC2a function with potential biomedical applications ranging from thrombosis to diabetes and cancer.
HostingRepositoryPRIDE
AnnounceDate2023-11-14
AnnouncementXMLSubmission_2023-11-14_08:55:52.732.xml
DigitalObjectIdentifier
ReviewLevelPeer-reviewed dataset
DatasetOriginOriginal dataset
RepositorySupportUnsupported dataset by repository
PrimarySubmitterPolina Prokofeva
SpeciesList scientific name: Homo sapiens (Human); NCBI TaxID: 9606;
ModificationListmonohydroxylated residue; iodoacetamide derivatized residue
InstrumentOrbitrap Fusion Lumos
Dataset History
RevisionDatetimeStatusChangeLog Entry
02022-03-14 11:18:00ID requested
12022-08-24 07:39:44announced
22023-11-14 08:55:53announced2023-11-14: Updated project metadata.
Publication List
Dataset with its publication pending
Keyword List
submitter keyword: pulldowns, PI3KC2a,Kinobeads
Contact List
Bernhard Kuster
contact affiliationChair of Proteomics and Bioanalytics, Technical University of Munich,Emil-Erlenmeyer-Forum 5, 85354 Freising, Germany
contact emailkuster@tum.de
lab head
Polina Prokofeva
contact affiliationChair of Proteomics and Bioanalytics, Technical University of Munich, Emil-Erlenmeyer-Forum 5, 85354 Freising, Germany
contact emailpolina.prokofeva@tum.de
dataset submitter
Full Dataset Link List
Dataset FTP location
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PRIDE project URI
Repository Record List
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