PXD007765-1

PXD007765 is an original dataset announced via ProteomeXchange.

Title	Dual protein kinase/ nucleoside kinase modulat ors for rationally designed polypharmacology
Description	Masitinib, a highly selective protein kinase inhibitor, can sensitise gemcitabine-refractory cancer cell lines when used in combination with gemcitabine. A reverse proteomic approach has identified the target responsible for this sensitisation: the deoxycytidine kinase (dCK). Masitinib, as well as other protein kinase inhibitors such as imatinib, interact with dCK and provoke an unforeseen conformational-dependent activation of this nucleoside kinase, modulating phosphorylation of nucleoside analogue drugs. This phenomenon leads to an increase of prodrug phosphorylation of most of the chemotherapeutic drugs activated by this nucleoside kinase. The unforeseen dual activity of protein kinase inhibition/nucleoside kinase activation could be of great therapeutic benefit, through either reducing toxicity of therapeutic agents by maintaining effectiveness at lower doses or by counteracting drug resistance initiated via down modulation of dCK target.
HostingRepository	PRIDE
AnnounceDate	2017-11-13
AnnouncementXML	Submission_2017-11-13_09:42:13.xml
DigitalObjectIdentifier
ReviewLevel	Peer-reviewed dataset
DatasetOrigin	Original dataset
RepositorySupport	Unsupported dataset by repository
PrimarySubmitter	AUDEBERT Stephane
SpeciesList	scientific name: Homo sapiens (Human); NCBI TaxID: 9606;
ModificationList	monohydroxylated residue; iodoacetamide derivatized residue
Instrument	LTQ Orbitrap Velos

Revision	Datetime	Status	ChangeLog Entry
0	2017-09-18 02:23:32	ID requested
⏵ 1	2017-11-13 09:42:14	announced
2	2024-10-22 04:41:08	announced	2024-10-22: Updated project metadata.

Hammam K, Saez-Ayala M, Rebuffet E, Gros L, Lopez S, Hajem B, Humbert M, Baudelet E, Audebert S, Betzi S, Lugari A, Combes S, Letard S, Casteran N, Mansfield C, Moussy A, De Sepulveda P, Morelli X, Dubreuil P, Dual protein kinase and nucleoside kinase modulators for rationally designed polypharmacology. Nat Commun, 8(1):1420(2017) [pubmed]

curator keyword: Biomedical

submitter keyword: Human, LTQ-Velos-Orbitrap, labelfree

Audebert Stephane
contact affiliation	MaP, Marseille Proteomique Centre de Recherche en Cancérologie de Marseille INSERM U1068/Institut Paoli-Calmettes 27, Bd Leï Roure, BP30059, 13273 Marseille CEDEX 9, France
contact email	stephane.audebert@inserm.fr
lab head
AUDEBERT Stephane
contact affiliation	Pharmacology department
contact email	stephane.audebert@inserm.fr
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/2017/11/PXD007765

PRIDE project URI

• PRIDE
  1. PXD007765
     1. Label: PRIDE project
     2. Name: Dual protein kinase/ nucleoside kinase modulat ors for rationally designed polypharmacology