PXD043204-2

PXD043204 is an original dataset announced via ProteomeXchange.

Title	T. brucei whole cell proteome changes upon exposure to the experimental phthalimide-based trypanocidal drug PHT-39
Description	In a phenotypic screening approach of novel molecules composed of a synergistic combination of phthalimide, benzimidazole, and triazole scaffolds we discovered compounds with potent anti-leishmanial activity. The resulting early-lead compound PHT-39, which contains a trifluoromethyl substitution, demonstrated the highest efficacy in a Leishmania infantum intramacrophage assay, with an EC50 of 1.2 +/- 3.2 μM.Cytotoxicity testing of PHT-39 in Hep-G2 cells indicated high selectivity of over 90-fold. To investigate the mechanism of action we carried out experiments in Trypanosoma brucei, which is also sensitive to PHT-39. Here we used liquid chromatography coupled with tandem mass spectrometry (LC-MSMS) to quantify the effects of PH-39 exposure on the global protein landscape in T. brucei.
HostingRepository	PRIDE
AnnounceDate	2024-10-22
AnnouncementXML	Submission_2024-10-22_06:32:55.672.xml
DigitalObjectIdentifier
ReviewLevel	Peer-reviewed dataset
DatasetOrigin	Original dataset
RepositorySupport	Unsupported dataset by repository
PrimarySubmitter	Martin Zoltner
SpeciesList	scientific name: Trypanosoma brucei; NCBI TaxID: 5691;
ModificationList	iodoacetamide derivatized residue
Instrument	Orbitrap Fusion

Revision	Datetime	Status	ChangeLog Entry
0	2023-06-22 04:36:16	ID requested
1	2024-03-12 11:27:06	announced
⏵ 2	2024-10-22 06:32:56	announced	2024-10-22: Updated project metadata.

10.1371/JOURNAL.PNTD.0012050;

submitter keyword: therapeutic agent, trypanosomes, leishmaniasis, mode of action, phthalimide

Martin Zoltner
contact affiliation	Charles University in Prague, BIOCEV Průmyslová 595 252 50 Vestec Czech Republic
contact email	zoltnerm@natur.cuni.cz
lab head
Martin Zoltner
contact affiliation	Division of Biological Chemistry & Drug Discovery School of Life Sciences University of Dundee Dundee DD1 5EH
contact email	m.zoltner@dundee.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/2024/03/PXD043204

PRIDE project URI

• PRIDE
  1. PXD043204
     1. Label: PRIDE project
     2. Name: T. brucei whole cell proteome changes upon exposure to the experimental phthalimide-based trypanocidal drug PHT-39