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PXD022021

PXD022021 is an original dataset announced via ProteomeXchange.

Dataset Summary
TitleChemically induced cereblon (CRBN) degradation: efficacy of recruiting CRBN in comparison to VHL
DescriptionAs small molecule degrader technology has developed, it has raised the question of whether E3 ligases could be induced to self-ubiquitinate. To examine this question, we generated six CRBN-CRBN degraders (also referred to as homo-PROTACs) and six CRBN-VHL degraders (hetero-PROTACs). From these compounds we identified two potent and selective CRBN degraders (ZXH-4-130 and ZXH-4-137), both of which are CRBN-VHL compounds. Comparison of these compounds to previously reported small molecule CRBN degraders further validated our observation that CRBN-VHL compounds are more potent degraders of CRBN than CRBN-CRBN compounds.
HostingRepositoryPRIDE
AnnounceDate2021-07-30
AnnouncementXMLSubmission_2021-07-29_23:46:48.245.xml
DigitalObjectIdentifier
ReviewLevelPeer-reviewed dataset
DatasetOriginOriginal dataset
RepositorySupportUnsupported dataset by repository
PrimarySubmitterEric Fischer
SpeciesList scientific name: Homo sapiens (Human); NCBI TaxID: 9606;
ModificationListmonohydroxylated residue; iodoacetamide derivatized residue
InstrumentOrbitrap Fusion Lumos
Dataset History
RevisionDatetimeStatusChangeLog Entry
02020-10-16 01:25:37ID requested
12021-07-29 23:46:48announced
Publication List
Dataset with its publication pending
Keyword List
submitter keyword: Cereblon (CRBN)
von Hippel-Lindau (VHL) protein
E3 ubiquitin ligases
small molecule degraders
PROTACs
targeted protein degradation
chemical probe
chemical biology
Contact List
Eric Fischer
contact affiliationDepartment of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA., Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA
contact emaileric_fischer@dfci.harvard.edu
lab head
Eric Fischer
contact affiliationDana-Farber Cancer Institute
contact emaileric_fischer@dfci.harvard.edu
dataset submitter
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Dataset FTP location
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