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PXD051199

PXD051199 is an original dataset announced via ProteomeXchange.

Dataset Summary
TitleDevelopment of novel chemical inhibitors of SETD8
DescriptionSETD8 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.
HostingRepositoryPRIDE
AnnounceDate2024-10-17
AnnouncementXMLSubmission_2024-10-17_08:35:40.856.xml
DigitalObjectIdentifier
ReviewLevelPeer-reviewed dataset
DatasetOriginOriginal dataset
RepositorySupportUnsupported dataset by repository
PrimarySubmitterRozbeh Jafari
SpeciesList scientific name: Homo sapiens (Human); NCBI TaxID: 9606;
ModificationListTMT6plex-126 reporter+balance reagent acylated residue; iodoacetamide derivatized residue
InstrumentQ Exactive HF
Dataset History
RevisionDatetimeStatusChangeLog Entry
02024-04-04 10:57:35ID requested
12024-10-17 08:35:41announced
Publication List
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]
Keyword List
submitter keyword: drug targets, thermal proteoome profiling,Cancer
Contact List
Rozbeh Jafari
contact affiliationKarolinska Institute, Department of Oncology-pathology
contact emailrozbeh.jafari@ki.se
lab head
Rozbeh Jafari
contact affiliationKarolinska Institutet
contact emailrozbeh.jafari@ki.se
dataset submitter
Full Dataset Link List
Dataset FTP location
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PRIDE project URI
Repository Record List
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