PXD069713-1

PXD069713 is an original dataset announced via ProteomeXchange.

Title	Characterization of novel Contilisant+Tubastatin A Multi-Target Small Molecules with against glioblastoma
Description	Glioblastoma is the most common and aggressive primary brain tumor in adults, with patient prognosis remaining poor. Treatment resistance and tumor recurrence are frequent, primarily due to the high intra- and inter-tumoral heterogeneity and the presence of glioma stem cells. Thus, there is an urgent need for novel and more effective therapeutic strategies. Multitarget small molecules (MSMs) are emerging as a novel therapeutic strategy for the treatment of complex diseases such as cancer. In the present work, we have generated a novel family of indole-based MSMs with pharmacophoric moieties combining the parent compounds Contilisant and HDAC inhibitor Tubastatin A. Thus, the MSMs were designed to inhibit monoamine oxidases (MAOs), cholinesterases (ChEs) and histone deacetylases (HDACs), while acting as histamine H3 receptor (H3R) antagonists and sigma 1 receptor (S1R) agonists. We generated 4 different molecules and we focused on evaluating the activity of the 2 most efficient MSM compounds against glioblastoma, both in vitro and in vivo. In silico analyses indicated that these compounds are theoretically capable of crossing the blood–brain barrier, while exhibiting low toxicity in healthy cells. OMICs-based analyses further revealed that the compounds induce dysregulation of the cell cycle and alter neurotransmission-related activity in glioma stem cells. In conclusion, our findings demonstrate the potential antitumor activity of these compounds in preclinical models of glioblastoma.
HostingRepository	PRIDE
AnnounceDate	2026-01-05
AnnouncementXML	Submission_2026-01-04_17:01:55.002.xml
DigitalObjectIdentifier
ReviewLevel	Peer-reviewed dataset
DatasetOrigin	Original dataset
RepositorySupport	Unsupported dataset by repository
PrimarySubmitter	Mikel Azkargorta
SpeciesList	scientific name: Homo sapiens (Human); NCBI TaxID: NEWT:9606;
ModificationList	No PTMs are included in the dataset
Instrument	timsTOF Pro

Revision	Datetime	Status	ChangeLog Entry
0	2025-10-21 01:24:48	ID requested
⏵ 1	2026-01-04 17:01:56	announced

10.3390/pharmaceutics17121594;

de Go, ñ, i I, Artetxe-Zurutuza A, Elizazu J, Garcia-Garcia de Garayo R, Vergara-Arce J, Azkargorta M, Toledano-Pinedo M, Porro-P, é, rez A, Elortza F, Marco-Contelles JL, Sampron N, Iturrioz-Rodriguez N, Matheu A, Generation and Characterization of Novel Contilisant+Tubastatin a Multitarget Small Molecules Against Glioblastoma. Pharmaceutics, 17(12):(2025) [pubmed]

submitter keyword: Glioblastoma, MSM, glioma stem cells, proliferation, HDAC inhibition

Felix Elortza
contact affiliation	CIC bioGUNE Proteomics Platform Bizkaia Tech. Park Build 800 Derio 48160 Spain
contact email	felortza@cicbiogune.es
lab head
Mikel Azkargorta
contact affiliation	Proteomics Platform CIC bioGUNE
contact email	mazkargorta@cicbiogune.es
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/2026/01/PXD069713

PRIDE project URI

• PRIDE
  1. PXD069713
     1. Label: PRIDE project
     2. Name: Characterization of novel Contilisant+Tubastatin A Multi-Target Small Molecules with against glioblastoma