PXD051199-1

PXD051199 is an original dataset announced via ProteomeXchange.

Title	Development of novel chemical inhibitors of SETD8
Description	SETD8 is a histone methyltransferase that catalyzes the monomethylation of histone H4K20. Overexpressed in cancer, several studies have suggested that it could be a potential target for treatment in certain tumors. However, there are currently very few SETD8 inhibitors, and all of them have bad pharmacological properties. Based on previously published structures of SETD8 bound to an H4K20me peptide, we have discovered a new chemical series of SETD8 inhibitors. As part of the characterization of these molecules, we conducted Thermal Proteome Profiling, aiming to discover potential additional targets as well as a better understanding of the signaling pathways that are affected by the drug.
HostingRepository	PRIDE
AnnounceDate	2024-10-17
AnnouncementXML	Submission_2024-10-17_08:35:40.856.xml
DigitalObjectIdentifier
ReviewLevel	Peer-reviewed dataset
DatasetOrigin	Original dataset
RepositorySupport	Unsupported dataset by repository
PrimarySubmitter	Rozbeh Jafari
SpeciesList	scientific name: Homo sapiens (Human); NCBI TaxID: 9606;
ModificationList	TMT6plex-126 reporter+balance reagent acylated residue; iodoacetamide derivatized residue
Instrument	Q Exactive HF

Revision	Datetime	Status	ChangeLog Entry
0	2024-04-04 10:57:35	ID requested
⏵ 1	2024-10-17 08:35:41	announced

10.1038/s41419-024-07106-6;

Murga M, Lopez-Pernas G, Soliva R, Fueyo-Marcos E, Amor C, Faustino I, Serna M, Serrano AG, D, í, az L, Mart, í, nez S, Blanco-Aparicio C, Ant, ó, n ME, Seashore-Ludlow B, Pastor J, Jafari R, Lafarga M, Llorca O, Orozco M, Fern, á, ndez-Capetillo O, SETD8 inhibition targets cancer cells with increased rates of ribosome biogenesis. Cell Death Dis, 15(9):694(2024) [pubmed]

submitter keyword: drug targets, thermal proteoome profiling,Cancer

Rozbeh Jafari
contact affiliation	Karolinska Institute, Department of Oncology-pathology
contact email	rozbeh.jafari@ki.se
lab head
Rozbeh Jafari
contact affiliation	Karolinska Institutet
contact email	rozbeh.jafari@ki.se
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/2024/10/PXD051199

PRIDE project URI

• PRIDE
  1. PXD051199
     1. Label: PRIDE project
     2. Name: Development of novel chemical inhibitors of SETD8