PXD058042

PXD058042 is an original dataset announced via ProteomeXchange.

Title	Characterization of a novel family of Contilisant+Bellinostat multitarget small molecules in glioblastoma
Description	Glioblastoma is the most common and malignant primary brain tumor in adults, with current treatment presenting limited effectiveness. Resistance to therapy is consequence of the high molecular and cellular heterogeneity. 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 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. For this, selected pharmacophoric moieties of the parent compounds Contilisant and HDAC inhibitor Belinostat were juxtaposed. 9 MSMs were synthesized and most of them exerted cytotoxic effect on glioma cells. Among them, 3 molecules were selected (MTP142, MTP156 and MTP150), and additional experiments revealed that they inhibited glioma stem cell (GSCs) activity, did not present toxicity and are expected to cross the BBB. In vivo and Omic studies were performed with MTP150 molecule, and results showed that it significantly reduced tumor growth in vivo, both alone and in combination with temozolomide (TMZ). Finally, transcriptomic and proteomic analyses on patient-derived GSCs revealed a deregulation in cell cycle and neurotransmission activity by the treatment with MTP150. In conclusion, our data reveal the efficacy of a novel family of MSMs in the pre-clinical setting of glioblastoma.
HostingRepository	PRIDE
AnnounceDate	2026-02-02
AnnouncementXML	Submission_2026-02-01_16:38:15.861.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	2024-11-19 05:00:41	ID requested
⏵ 1	2026-02-01 16:38:16	announced

Artetxe-Zurutuza A, Iturrioz-Rodriguez N, Elizazu J, Garcia-Garcia de Garayo R, de Go, ñ, i I, Vergara J, Toledano-Pinedo M, Porro-P, é, rez A, Azkargorta M, Elortza F, Marco-Contelles JL, Sampron N, Matheu A, of a Novel Family of Contilisant + Belinostat Multitarget Small Molecules in Glioblastoma. Pharmaceuticals (Basel), 19(1):(2025) [pubmed]

10.3390/ph19010020;

submitter keyword: glioblastoma,MSM, DDI199, HDAC

Felix Elortza
contact affiliation	Proteomics Platform CIDC bioGUNE Bizkaia Tech. Park Build. 800 48160 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/2026/02/PXD058042

PRIDE project URI

• PRIDE
  1. PXD058042
     1. Label: PRIDE project
     2. Name: Characterization of a novel family of Contilisant+Bellinostat multitarget small molecules in glioblastoma