<<< Full experiment listing

PXD037895-1

PXD037895 is an original dataset announced via ProteomeXchange.

Dataset Summary
TitleA Selective Small-Molecule STAT5 PROTAC Degrader Capable of Achieving Tumor Regression In Vivo
DescriptionThe signal transducer and activator of transcription 5 (STAT5) is an attractive therapeutic target but successful targeting of STAT5 has proved to be difficult. We report herein the development of AK-2292 as a first, potent and selective small-molecule degrader of both STAT5A and STAT5B isoforms. AK-2292 induces degradation of STAT5A/B proteins with an outstanding selectivity over all other STAT proteins and >6,000 non-STAT proteins, leading to selective inhibition of STAT5 activity in cells. AK-2292 effectively induces STAT5 depletion in normal mouse tissues and human chronic myeloid leukemia (CML) xenograft tissues and achieves tumor regression in two CML xenograft mouse models at well-tolerated dose-schedules. AK-2292 is not only a powerful research tool with which to investigate the biology of STAT5 and therapeutic potential of selective STAT5 protein depletion and inhibition in vitro and in vivo, but also a promising lead compound toward ultimate development of a STAT5-targeted therapy.
HostingRepositoryPRIDE
AnnounceDate2023-01-25
AnnouncementXMLSubmission_2023-01-25_09:02:18.180.xml
DigitalObjectIdentifier
ReviewLevelPeer-reviewed dataset
DatasetOriginOriginal dataset
RepositorySupportUnsupported dataset by repository
PrimarySubmitterLongchuan Bai
SpeciesList scientific name: Homo sapiens (Human); NCBI TaxID: 9606;
ModificationListTMT6plex-126 reporter+balance reagent acylated residue; monohydroxylated residue; deamidated residue; iodoacetamide derivatized residue
InstrumentOrbitrap Fusion
Dataset History
RevisionDatetimeStatusChangeLog Entry
02022-11-03 04:06:32ID requested
12023-01-25 09:02:18announced
Publication List
Dataset with its publication pending
Keyword List
submitter keyword: TMT proteomics,STAT5, PROTAC
Contact List
ShaomengWang
contact affiliation2Departments of Internal Medicine, University of Michigan, Ann Arbor MI 48109, USA.
contact emailshaomeng@umich.edu
lab head
Longchuan Bai
contact affiliationUniversity of Michigan
contact emaillbai@med.umich.edu
dataset submitter
Full Dataset Link List
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/2023/01/PXD037895
PRIDE project URI
Repository Record List
[ + ]