PXD033239

PXD033239 is an original dataset announced via ProteomeXchange.

Title	Novel, highly potent PROTACs targeting AURORA-A kinase
Description	The family of AURORA kinases is essential for cell cycle progression and dysregulation of AURORA-A in cancer led to a large number of clinical and pre-clinical inhibitors. However, ATP competitive AURORA-A inhibitors usually do not target non-catalytic functions that have also been identified as mechanisms promoting tumorigenesis. To target non-catalytic as well as catalytic functions, we developed a series of PROTACs (PROteolysis targeting chimeras) based on the selective AURORA-A kinase inhibitor MK-5108 (VX-689) and the CEREBLON E3-ligase ligands. The most potent PROTAC, JB301, had good physicochemical properties and cell penetration resulting in degradation of AURORA-A in leukemic cells at single digit nM concentration. In the presented datasets, we determined the intracellular degradation specificity of the AURKA PROTAC JB300. We therefore treated MV4-11 cells with JB300 and the corresponding ligand MK-5108, or DMSO and quantified the induced degradation using a label free approach.
HostingRepository	PRIDE
AnnounceDate	2023-11-14
AnnouncementXML	Submission_2023-11-14_08:49:05.185.xml
DigitalObjectIdentifier
ReviewLevel	Peer-reviewed dataset
DatasetOrigin	Original dataset
RepositorySupport	Unsupported dataset by repository
PrimarySubmitter	Nicola Berner
SpeciesList	scientific name: Homo sapiens (Human); NCBI TaxID: 9606;
ModificationList	acetylated residue; monohydroxylated residue; iodoacetamide derivatized residue
Instrument	Q Exactive HF-X

Revision	Datetime	Status	ChangeLog Entry
0	2022-04-14 05:19:25	ID requested
1	2023-09-14 09:53:34	announced
⏵ 2	2023-11-14 08:49:05	announced	2023-11-14: Updated project metadata.

Dataset with its publication pending

submitter keyword: LC-MSMS, AURKA,PROTAC, Protein degrader

Bernhard Kuster
contact affiliation	Technical University of Munich, Chair of Proteomics and Bioanalytics, Emil-Erlenmeyer-Forum 5, 85354 Freising, Germany
contact email	kuster@tum.de
lab head
Nicola Berner
contact affiliation	German Cancer Consortium (DKTK), Germany Chair of Proteomics and Bioanalytics Technical University of Munich (TUM), Freising, Germany German Cancer Research Center (DKFZ), Heidelberg, Germany
contact email	n.berner@tum.de
dataset submitter

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PRIDE project URI

• PRIDE
  1. PXD033239
     1. Label: PRIDE project
     2. Name: Novel, highly potent PROTACs targeting AURORA-A kinase