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PXD035398-1

PXD035398 is an original dataset announced via ProteomeXchange.

Dataset Summary
TitleDiptoindonesin G is a middle domain HSP90 modulator for cancer treatment
DescriptionHSP90 inhibitors can target many oncoproteins simultaneously, but none have made it through clinical trials due to dose-limiting toxicity and induction of heat shock response, leading to clinical resistance. We identified diptoindonesin G (dip G) as an HSP90 modulator that can promote degradation of HSP90 clients by binding to the middle domain of HSP90 without inducing heat shock response. Although dip G does not bind to the ligand binding domain (LBD) of estrogen receptor (ER), it promotes degradation of ER in breast cancer cells. We further showed that treatment of ER LBD mutantexpressing cells with dip G promoted degradation of wild type and mutant ER with similar efficacy, downregulated ER-regulated gene expression, and inhibited cell proliferation. Our data suggest that dip G circumvents some obstacles associated with HSP90 inhibition and may be developed as a new therapeutic avenue to various cancers, particularly endocrine resistant breast cancer harboring ESR1 mutations
HostingRepositoryPRIDE
AnnounceDate2022-11-16
AnnouncementXMLSubmission_2022-11-16_12:23:37.431.xml
DigitalObjectIdentifier
ReviewLevelPeer-reviewed dataset
DatasetOriginOriginal dataset
RepositorySupportUnsupported dataset by repository
PrimarySubmitterMinMa
SpeciesList scientific name: Homo sapiens (Human); NCBI TaxID: 9606;
ModificationListNo PTMs are included in the dataset
InstrumentOrbitrap Fusion Lumos
Dataset History
RevisionDatetimeStatusChangeLog Entry
02022-07-20 00:11:56ID requested
12022-11-16 12:23:37announced
22023-11-14 08:57:30announced2023-11-14: Updated project metadata.
Publication List
Keyword List
submitter keyword: ESR1
HSP90
heat shock
LBD mutations
diptoindonesin G
HSP90 inhibitor
Y537S
HSP90 middle domain
ER alpha
Contact List
WeiXu
contact affiliationMarian A. Messerschmidt Professor of Oncology Associate Director, McArdle Laboratory for Cancer Research,UW Madison
contact emailwxu@oncology.wisc.edu
lab head
MinMa
contact affiliationUW madison
contact emailmma58@wisc.edu
dataset submitter
Full Dataset Link List
Dataset FTP location
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PRIDE project URI
Repository Record List
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