PXD038022

PXD038022 is an original dataset announced via ProteomeXchange.

Title	DIA-MS Detect the Targeted EGFR Dephosphorylation by Phosphorylation Targeting Chimera (PhosTAC)
Description	Epidermal growth factor receptor (EGFR) is an important receptor tyrosine kinase protein. Activated EGFR promotes downstream signal transductions through phosphorylation, and its phosphorylation has been implicated in pathologies including many types of cancers. Previously, our lab has developed the phosphorylation targeting chimera (PhosTAC) to achieve targeted dephosphorylation of proteins of interest. In this study, harnessing a tyrosine phosphatase (PTPN2) for the first time, we designed and synthesized a series of PhosTACs to dephosphorylate wild-type and mutant EGFR. We demonstrated efficient EGFR dephosphorylation with the treatment of PhosTACs. Phosphoproteomics was used to confirm PhosTAC induced dephosphorylation as well as its different inhibitory patterns from the warhead gefitinib. Consistent with EGFR dephosphorylation, EGFR PhosTACs induced apoptosis and inhibited cell proliferation. As RTKs are critical receptors for cellular signaling and targeted therapies, these tyrosine-phosphatase recruiting PhosTACs showcased their potential of modulating RTKs, expanding the scope of bifunctional molecules utility.
HostingRepository	PRIDE
AnnounceDate	2024-04-03
AnnouncementXML	Submission_2024-04-02_19:12:27.184.xml
DigitalObjectIdentifier
ReviewLevel	Peer-reviewed dataset
DatasetOrigin	Original dataset
RepositorySupport	Unsupported dataset by repository
PrimarySubmitter	Wenxue Li
SpeciesList	scientific name: Homo sapiens (Human); NCBI TaxID: 9606;
ModificationList	phosphorylated residue; acetylated residue; monohydroxylated residue; iodoacetamide derivatized residue
Instrument	Orbitrap Fusion Lumos

Revision	Datetime	Status	ChangeLog Entry
0	2022-11-07 10:13:27	ID requested
⏵ 1	2024-04-02 19:12:27	announced

Dataset with its publication pending

submitter keyword: Phosphoproteomics,DIA-MS, PhosTAC, EGFR, Kinase

Yansheng Liu
contact affiliation	Yale Cancer Biology Institute
contact email	yansheng.liu@yale.edu
lab head
Wenxue Li
contact affiliation	Yale University
contact email	wenxue.li@yale.edu
dataset submitter

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/2024/04/PXD038022

PRIDE project URI

• PRIDE
  1. PXD038022
     1. Label: PRIDE project
     2. Name: DIA-MS Detect the Targeted EGFR Dephosphorylation by Phosphorylation Targeting Chimera (PhosTAC)