PXD055063

PXD055063 is an original dataset announced via ProteomeXchange.

Title	Exploiting the DCAF16-SPIN4 interaction to identify DCAF16 ligands for PROTAC development
Description	Traditional small molecule drugs often target protein activity directly, but challenges arise when proteins lack suitable functional sites. An alternative approach is targeted protein degradation (TPD), which directs proteins to cellular machinery for proteolytic degradation. Recent studies have identified new E3 ligases, expanding the potential of TPD. Among these, DCAF16 has shown promise in facilitating protein degradation through both PROTAC and molecular glue mechanisms. In this study, we developed a Homogeneous Time Resolved Fluorescence (HTRF) assay to identify additional DCAF16 ligands using an in-house electrophile library. This led to the identification of two diastereomeric compounds, with one engaging DCAF16 at cysteines C177-179 and another reducing its expression. We demonstrated that the compound engaging DCAF16 can be transformed into a PROTAC capable of degrading FKBP12.
HostingRepository	PRIDE
AnnounceDate	2024-12-06
AnnouncementXML	Submission_2024-12-06_07:20:58.474.xml
DigitalObjectIdentifier
ReviewLevel	Peer-reviewed dataset
DatasetOrigin	Original dataset
RepositorySupport	Unsupported dataset by repository
PrimarySubmitter	Xiaoyu Zhang
SpeciesList	scientific name: Homo sapiens (Human); NCBI TaxID: 9606;
ModificationList	TMT6plex-126 reporter+balance reagent acylated residue
Instrument	Orbitrap Eclipse

Revision	Datetime	Status	ChangeLog Entry
0	2024-08-22 06:11:55	ID requested
⏵ 1	2024-12-06 07:20:58	announced

10.1039/D4MD00681J;

submitter keyword: HTRF, DCAF16, PROTAC

Xiaoyu Zhang
contact affiliation	Northwestern University, Department of Chemistry
contact email	zhang@northwestern.edu
lab head
Xiaoyu Zhang
contact affiliation	Northwestern University
contact email	zhang@northwestern.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/2024/12/PXD055063

PRIDE project URI

• PRIDE
  1. PXD055063
     1. Label: PRIDE project
     2. Name: Exploiting the DCAF16-SPIN4 interaction to identify DCAF16 ligands for PROTAC development