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PXD057836

PXD057836 is an original dataset announced via ProteomeXchange.

Dataset Summary
TitleSynthesis and Anti-mycobacterial Activity of Novel Medium-chain β-Lactone Derivatives: A Multi-Target Strategy to combat Mycobacterium abscessus and other Pathogenic Mycobacteria
DescriptionTargeting the enzymes involved in mycobacterial lipid metabolism; which are mainly serine and cysteine enzymes (i.e., (Ser/Cys)-based enzymes; has emerged as a promising strategy to combat not only M. tuberculosis, but also other chronic non-tuberculous mycobacterial infections like those caused by M. marinum or M. abscessus. Among the known inhibitors of such mycobacterial enzymes, β-lactones represent promising candidates for the development of new derivatives that target lipid-processing enzymes critical for mycobacterial growth and survival. In this context, a new set of 38 lipophilic β lactone derivatives have been synthesized and tested for their anti-mycobacterial activities against the three aforementioned pathogenic mycobacteria. Remarkably, the determined MIC revealed that some VM β-lactones were able to inhibit M. abscessus growth in vitro in culture broth medium and/or inside infected macrophages. In addition, using a competitive activity-based protein profiling approach, the potential target enzymes of VM043, the most active inhibitor of extracellular bacterial growth, were further identified; thus, confirming the multi-target nature of this family of molecules.
HostingRepositoryPRIDE
AnnounceDate2025-04-23
AnnouncementXMLSubmission_2025-04-22_23:17:04.906.xml
DigitalObjectIdentifier
ReviewLevelPeer-reviewed dataset
DatasetOriginOriginal dataset
RepositorySupportUnsupported dataset by repository
PrimarySubmitterAUDEBERT Stephane
SpeciesList scientific name: Mycobacterium tuberculosis; NCBI TaxID: NCBITaxon:1773; scientific name: Bacteria; NCBI TaxID: NCBITaxon:2; scientific name: Mycobacteroides abscessus subsp. abscessus; NCBI TaxID: 1185650;
ModificationListmonohydroxylated residue; iodoacetamide derivatized residue
InstrumentQ Exactive Plus
Dataset History
RevisionDatetimeStatusChangeLog Entry
02024-11-13 03:48:21ID requested
12025-04-22 23:17:05announced
Publication List
Dataset with its publication pending
Keyword List
submitter keyword: Activity-based protein profiling
multitarget inhibitor-like affinity-based probes
drug susceptibility
intracellular activity
proteomic analysis
mycobacteria
LC-MSMS
Contact List
Dr CAVALIER Jean-François
contact affiliationLipolysis and bacterial Pathogenicity Team LISM UMR7255 CNRS 31, chemin Joseph Aiguier - CS 70071 F-13402 marseille cedex 09
contact emailjfcavalier@imm.cnrs.fr
lab head
AUDEBERT Stephane
contact affiliationMarseille Proteomic, Centre de Recherche en Cancérologie de Marseille, Inserm UMR1068, CNRS UMR7258, Aix Marseille Université U105, Institut Paoli Calmettes, 27 Boulevard Leï Roure CS30059 13273 Marseille Cedex 09 France
contact emailstephane.audebert@inserm.fr
dataset submitter
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Dataset FTP location
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