PXD034776

PXD034776 is an original dataset announced via ProteomeXchange.

Title	Drug Affinity Responsive Target Stability unveils Filamins as biological targets for Artemetin, an anti-cancer flavonoid.
Description	Artemetin is a valuable 5-hydroxy-3,6,7,3',4'-pentamethoxyflavone found in many different medicinal plants with a very good oral bioavailability and drug-likeness values endowed with numerous bioactivities such as anti-inflammatory and anti-cancer ones. Here, a multi-disciplinary strategy has been developed and applied for identifying Artemetin target(s) to fully address its mechanism of action, based on drug affinity response target stability and targeted limited proteolysis. Both approaches point to the identification of Filamins A and B as major Artemetin targets in HeLa cell lysates, giving also detailed insights into the ligand/proteins interaction sites. Interestingly, also the 8-prenyl-Artemetin, which is a more permeable semisynthetic analog, directly interacts with Filamin A and B. Both compounds alter filamins conformation in living HeLa cells with an effect on cytoskeleton disassembly and on the disorganization of the F-actin filaments, mediated by the dissociation of filamins. Both the natural compound and its derivative are able to block cell migration, expectantly acting on tumor metastasis’s occurrence and development.
HostingRepository	PRIDE
AnnounceDate	2023-11-14
AnnouncementXML	Submission_2023-11-14_08:16:43.073.xml
DigitalObjectIdentifier
ReviewLevel	Peer-reviewed dataset
DatasetOrigin	Original dataset
RepositorySupport	Unsupported dataset by repository
PrimarySubmitter	Maria Chiara Monti
SpeciesList	scientific name: Homo sapiens (Human); NCBI TaxID: 9606;
ModificationList	iodoacetamide derivatized residue
Instrument	Q Exactive

Revision	Datetime	Status	ChangeLog Entry
0	2022-06-21 04:17:11	ID requested
1	2022-10-13 21:53:08	announced
⏵ 2	2023-11-14 08:16:43	announced	2023-11-14: Updated project metadata.

Ferraro G, Belvedere R, Petrella A, Tosco A, Stork B, Salamone S, Minassi A, Pollastro F, Morretta E, Monti MC, Drug affinity-responsive target stability unveils filamins as biological targets for artemetin, an anti-cancer flavonoid. Front Mol Biosci, 9():964295(2022) [pubmed]

submitter keyword: Anti-Cancer.,Bioactive Natural Compounds, Drug Affinity Responsive Target Stability, Cytoskeleton, Proteomics

Maria Chiara Monti
contact affiliation	Department of Pharmacy, Università di Salerno, Via Giovanni Paolo II 132, Fisciano, 84084 Salerno, Italy
contact email	mcmonti@unisa.it
lab head
Maria Chiara Monti
contact affiliation	Dept Pharmacy University of Salerno
contact email	mcmonti@unisa.it
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/2022/10/PXD034776

PRIDE project URI

• PRIDE
  1. PXD034776
     1. Label: PRIDE project
     2. Name: Drug Affinity Responsive Target Stability unveils Filamins as biological targets for Artemetin, an anti-cancer flavonoid.