PXD048953
PXD048953 is an original dataset announced via ProteomeXchange.
Dataset Summary
Title | Identification of a Novel Ferroptosis Inducer with Dual Modulatory Effects on GPX4 Activity and Stability |
Description | Ferroptosis is a unique form of intracellular iron-dependent cell death that differs from apoptosis, necrosis, and autophagy. GPX4, an antioxidant defense enzyme, plays a pivotal role as regulator of ferroptosis. Extensive researches suggest that targeting GPX4 holds promise for cancer therapy. However, the current GPX4 inhibitors face challenges due to unfavorable drug-like properties, which hinder their progress in clinical development. In this study, we identified a novel inhibitor called MI-2, demonstrating potent ferroptosis-inducing capacity. Mechanistically, MI-2 effectively inhibits the activity of GPX4 by direct interaction. Furthermore, MI-2 promotes the degradation of GPX4 through its well-established target, MALT1. In multiple cancer models, MI-2 has demonstrated synergistic effects when combined with sorafenib or regorafenib, resulting in enhanced ferroptosis induction. These findings highlight the dual modulatory effects of MI-2 on GPX4 activity and stability, offering a promising starting point for the development of drug-like GPX4 inhibitors with translational potential. |
HostingRepository | iProX |
AnnounceDate | 2024-01-27 |
AnnouncementXML | Submission_2024-04-22_18:48:06.202.xml |
DigitalObjectIdentifier | |
ReviewLevel | Peer-reviewed dataset |
DatasetOrigin | Original dataset |
RepositorySupport | Unsupported dataset by repository |
PrimarySubmitter | Bo Yang |
SpeciesList | scientific name: Homo sapiens; NCBI TaxID: 9606; |
ModificationList | No PTMs are included in the dataset |
Instrument | Q Exactive |
Dataset History
Revision | Datetime | Status | ChangeLog Entry |
---|---|---|---|
0 | 2024-01-28 20:16:13 | ID requested | |
⏵ 1 | 2024-04-22 18:48:06 | announced |
Publication List
Dataset with its publication pending |
Keyword List
submitter keyword: Ferroptosis, MI-2, GPX4 |
Contact List
Cun Wang | |
---|---|
contact affiliation | Shanghai Jiao Tong University |
contact email | cwang@shsci.org |
lab head | |
Bo Yang | |
contact affiliation | East China Normal University |
contact email | yangbo6674@163.com |
dataset submitter |
Full Dataset Link List
iProX dataset URI |