PXD023036

PXD023036 is an original dataset announced via ProteomeXchange.

Title	ABPP-HT - high-throughput activity-based profiling of deubiquitylating enzyme inhibitors in a cellular context
Description	The potency and selectivity of a small molecule inhibitor are key parameters to assess during the early stages of drug discovery. In particular, it is very informative for characterizing compounds in a relevant cellular context in order to reveal potential off-target effects and drug efficacy. Activity-based probes (ABPs) are valuable tools for that purpose, however, obtaining cellular target engagement data in a high-throughput format has been particularly challenging. Here, we describe a new methodology named ABPP-HT (high-throughput-compatible activity-based protein profiling), implementing a semi-automated proteomic sample preparation workflow that increased the throughput capabilities of the classical ABPP workflow approximately ten times while preserving its enzyme profiling characteristics. Using a panel of deubiquitylating enzyme (DUB) inhibitors, we demonstrate the feasibility of ABPP-HT to provide compound selectivity profiles of endogenous DUBs in a cellular context at a fraction of time as compared to previous methodologies
HostingRepository	PRIDE
AnnounceDate	2021-02-24
AnnouncementXML	Submission_2021-02-23_22:51:57.351.xml
DigitalObjectIdentifier
ReviewLevel	Peer-reviewed dataset
DatasetOrigin	Original dataset
RepositorySupport	Unsupported dataset by repository
PrimarySubmitter	Raphael A Heilig
SpeciesList	scientific name: Mus musculus (Mouse); NCBI TaxID: 10090; scientific name: Homo sapiens (Human); NCBI TaxID: 9606;
ModificationList	monohydroxylated residue; iodoacetamide derivatized residue
Instrument	timsTOF Pro; Q Exactive

Revision	Datetime	Status	ChangeLog Entry
0	2020-12-10 00:14:36	ID requested
⏵ 1	2021-02-23 22:51:57	announced

Dataset with its publication pending

submitter keyword: activitomics, activity-based probes, deubiquitylating enzymes, ubiquitin, drug discovery, pharmacology, automation

Roman Fischer
contact affiliation	Dr. Roman Fischer Associate Professor and Head of Discovery Proteomics Facility University of Oxford Target Discovery Institute, NDMRB Roosevelt Drive Oxford, OX3 7FZ United Kingdom
contact email	roman.fischer@ndm.ox.ac.uk
lab head
Raphael A Heilig
contact affiliation	University of Oxford
contact email	raphael.heilig@ndm.ox.ac.uk
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/2021/02/PXD023036

PRIDE project URI

• PRIDE
  1. PXD023036
     1. Label: PRIDE project
     2. Name: ABPP-HT - high-throughput activity-based profiling of deubiquitylating enzyme inhibitors in a cellular context