PXD039385 is an
original dataset announced via ProteomeXchange.
Dataset Summary
Title | Piperlongumine (PL) conjugates induce targeted protein degradation |
Description | PROteolysis Targeting Chimeras (PROTACs) are bifunctional molecules that degrade target proteins through recruiting E3 ligases. However, their application is limited in part because few E3 ligases can be recruited by known E3 ligase ligands. In this study, we identified piperlongumine (PL), a natural product, as a covalent E3 ligase recruiter, which induces CDK9 degradation when it is conjugated with SNS-032, a CDK9 inhibitor. To evaluate the specificity of the PL-SNS-032 lead conjugate named 955, TMT-based proteomics were conducted to compare 955 with its warhead SNS-032 in MOLT4 cells. As expected, cells exhibited a significant reduction of CDK9 after treatment with 0.1 µM 955 for 1 h and 6 h while treatment with 1 µM SNS-032 for 6 h had no significant effect on CDK9. Interestingly, 955, but not SNS-032, can also potently degrade CDK10. |
HostingRepository | PRIDE |
AnnounceDate | 2024-05-24 |
AnnouncementXML | Submission_2024-05-24_01:01:56.417.xml |
DigitalObjectIdentifier | |
ReviewLevel | Peer-reviewed dataset |
DatasetOrigin | Original dataset |
RepositorySupport | Unsupported dataset by repository |
PrimarySubmitter | Dongwen Lyu |
SpeciesList | scientific name: Homo sapiens (Human); NCBI TaxID: 9606; |
ModificationList | No PTMs are included in the dataset |
Instrument | Orbitrap Fusion Lumos |
Dataset History
Revision | Datetime | Status | ChangeLog Entry |
0 | 2023-01-13 05:36:20 | ID requested | |
⏵ 1 | 2024-05-24 01:01:57 | announced | |
Publication List
Pei J, Xiao Y, Liu X, Hu W, Sobh A, Yuan Y, Zhou S, Hua N, Mackintosh SG, Zhang X, Basso KB, Kamat M, Yang Q, Licht JD, Zheng G, Zhou D, Lv D, Piperlongumine conjugates induce targeted protein degradation. Cell Chem Biol, 30(2):203-213.e17(2023) [pubmed] |
10.1016/j.chembiol.2023.01.004; |
Keyword List
submitter keyword: Piperlongumine, PROTAC, E3 ligase, CDK9 |
Contact List
Dongwen Lv |
contact affiliation | Department of Biochemistry and Structural Biology and Center for Innovative Drug Discovery School of Medicine, University of Texas Health Science Center at San Antonio, 7703 Floyd Curl Drive, San Antonio, TX 78229, United States |
contact email | lyud@uthscsa.edu |
lab head | |
Dongwen Lyu |
contact affiliation | UT Health San Antonio |
contact email | lyud@uthscsa.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/2024/05/PXD039385 |
PRIDE project URI |
Repository Record List
[ + ]
[ - ]
- PRIDE
- PXD039385
- Label: PRIDE project
- Name: Piperlongumine (PL) conjugates induce targeted protein degradation