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PXD018674

PXD018674 is an original dataset announced via ProteomeXchange.

Dataset Summary
TitlePROTAC-triggered degradation of MYC
DescriptionThe oncogene MYC drives many cancers and is an outstanding therapeutic target. MYC is an intrinsically disordered protein, and therefore, targeting MYC remains a challenge. Here, we developed a proteolysis targeting chimera (PROTAC) degrading MYC: MDEG-541. The inhibitor is based on the MYC-MAX dimerization inhibitor 10058-F4 and Thalidomide. Mode of action depends on the proteasome and cereblon. MDEG-541 shows single digit mM activity in most sensitive colon and pancreatic cancer cell lines as well as gastrointestinal tumor organoids.
HostingRepositoryPRIDE
AnnounceDate2022-05-12
AnnouncementXMLSubmission_2022-05-11_21:17:54.579.xml
DigitalObjectIdentifier
ReviewLevelPeer-reviewed dataset
DatasetOriginOriginal dataset
RepositorySupportUnsupported dataset by repository
PrimarySubmitterStephanie Heinzlmeir
SpeciesList scientific name: Homo sapiens (Human); NCBI TaxID: 9606;
ModificationListiodoacetamide derivatized residue
InstrumentOrbitrap Fusion Lumos
Dataset History
RevisionDatetimeStatusChangeLog Entry
02020-04-20 06:25:19ID requested
12022-05-11 21:17:55announced
Publication List
Lier S, Sellmer A, Orben F, Heinzlmeir S, Krau, ß L, Schneeweis C, Hassan Z, Schneider C, Patricia Gloria Sch, ä, fer A, Pongratz H, Engleitner T, Ö, llinger R, Kuisl A, Bassermann F, Schlag C, Kong B, Dove S, Kuster B, Rad R, Reichert M, Wirth M, Saur D, Mahboobi S, Schneider G, A novel Cereblon E3 ligase modulator with antitumor activity in gastrointestinal cancer. Bioorg Chem, 119():105505(2022) [pubmed]
Keyword List
submitter keyword: human, MYC degradation, LC-MS3
Contact List
Prof. Dr. Bernhard Kuster
contact affiliationTechnical University of Munich Chair of Proteomics and Bioanalytics Emil-Erlenmeyer-Forum 5 85354 Freising Germany
contact emailkuster@tum.de
lab head
Stephanie Heinzlmeir
contact affiliationChair of Proteomics and Bioanalytics, Technische Universität München, Germany
contact emailstephanie.heinzlmeir@tum.de
dataset submitter
Full Dataset Link List
Dataset FTP location
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PRIDE project URI
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