PXD032284-2

PXD032284 is an original dataset announced via ProteomeXchange.

Title	Kinobead profiling of PITCOINs1-3
Description	Phosphatidylinositol 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.
HostingRepository	PRIDE
AnnounceDate	2023-11-14
AnnouncementXML	Submission_2023-11-14_08:55:52.732.xml
DigitalObjectIdentifier
ReviewLevel	Peer-reviewed dataset
DatasetOrigin	Original dataset
RepositorySupport	Unsupported dataset by repository
PrimarySubmitter	Polina Prokofeva
SpeciesList	scientific name: Homo sapiens (Human); NCBI TaxID: 9606;
ModificationList	monohydroxylated residue; iodoacetamide derivatized residue
Instrument	Orbitrap Fusion Lumos

Revision	Datetime	Status	ChangeLog Entry
0	2022-03-14 11:18:00	ID requested
1	2022-08-24 07:39:44	announced
⏵ 2	2023-11-14 08:55:53	announced	2023-11-14: Updated project metadata.

Dataset with its publication pending

submitter keyword: pulldowns, PI3KC2a,Kinobeads

Bernhard Kuster
contact affiliation	Chair of Proteomics and Bioanalytics, Technical University of Munich,Emil-Erlenmeyer-Forum 5, 85354 Freising, Germany
contact email	kuster@tum.de
lab head
Polina Prokofeva
contact affiliation	Chair of Proteomics and Bioanalytics, Technical University of Munich, Emil-Erlenmeyer-Forum 5, 85354 Freising, Germany
contact email	polina.prokofeva@tum.de
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/2022/08/PXD032284

PRIDE project URI

• PRIDE
  1. PXD032284
     1. Label: PRIDE project
     2. Name: Kinobead profiling of PITCOINs1-3