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PXD048854

PXD048854 is an original dataset announced via ProteomeXchange.

Dataset Summary
TitleTargeting protein tyrosine phosphatase non-receptor type 2 with a novel inhibitor for the treatment of acute myeloid leukemia
DescriptionAcute myeloid leukemia (AML) is a fatal disease characterized by a bleak prognosis. For over four decades, treatment options for AML have been constrained to administering high-dose cytotoxic chemotherapy. However, the emergence of drug resistance and the resultant toxic side effects have created an urgent necessity for identifying novel therapeutic targets. In this study, non-receptor protein tyrosine phosphatase type 2 (PTPN2) is highly expressed in AML. Remarkably, knock down of PTPN2 expression markedly mitigated AML burden both in vitro and in vivo. Additionally, we unveiled the direct interaction between PTPN2 and C-MYC, establishing C-MYC as a direct acting substrate of PTPN2. Then, we performed a small-molecule compound screening to identify K73, a selective inhibitor of PTPN2. At the same time, K73 showed a good safety profile and exhibited strong activity against AML in vivo. In conclusion, we have pinpointed a considerable therapeutic potential in targeting PTPN2 for AML treatment and discovered a novel class of selective PTPN2 inhibitors suitable for AML therapy.
HostingRepositoryiProX
AnnounceDate2024-01-24
AnnouncementXMLSubmission_2024-01-24_18:38:40.083.xml
DigitalObjectIdentifier
ReviewLevelPeer-reviewed dataset
DatasetOriginOriginal dataset
RepositorySupportUnsupported dataset by repository
PrimarySubmitterWenbin Kuang
SpeciesList scientific name: Homo sapiens; NCBI TaxID: 9606;
ModificationListNo PTMs are included in the dataset
InstrumentOrbitrap Fusion
Dataset History
RevisionDatetimeStatusChangeLog Entry
02024-01-24 18:36:22ID requested
12024-01-24 18:38:40announced
Publication List
Dataset with its publication pending
Keyword List
submitter keyword: PTPN2, C-MYC, acute myeloid leukemia, cell cycle, small molecule inhibitor
Contact List
Peng Yang
contact affiliationChina Pharmaceutical University
contact emailpengyang@cpu.edu.cn
lab head
Wenbin Kuang
contact affiliationChina Pharmaceutical University
contact email1520220107@cpu.edu.cn
dataset submitter
Full Dataset Link List
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