PXD057836 is an
original dataset announced via ProteomeXchange.
Dataset Summary
Title | Synthesis and Anti-mycobacterial Activity of Novel Medium-chain β-Lactone Derivatives: A Multi-Target Strategy to combat Mycobacterium abscessus and other Pathogenic Mycobacteria |
Description | Targeting 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. |
HostingRepository | PRIDE |
AnnounceDate | 2025-04-23 |
AnnouncementXML | Submission_2025-04-22_23:17:04.906.xml |
DigitalObjectIdentifier | |
ReviewLevel | Peer-reviewed dataset |
DatasetOrigin | Original dataset |
RepositorySupport | Unsupported dataset by repository |
PrimarySubmitter | AUDEBERT 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; |
ModificationList | monohydroxylated residue; iodoacetamide derivatized residue |
Instrument | Q Exactive Plus |
Dataset History
Revision | Datetime | Status | ChangeLog Entry |
0 | 2024-11-13 03:48:21 | ID requested | |
⏵ 1 | 2025-04-22 23:17:05 | announced | |
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 affiliation | Lipolysis and bacterial Pathogenicity Team LISM UMR7255 CNRS 31, chemin Joseph Aiguier - CS 70071 F-13402 marseille cedex 09 |
contact email | jfcavalier@imm.cnrs.fr |
lab head | |
AUDEBERT Stephane |
contact affiliation | Marseille 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 email | stephane.audebert@inserm.fr |
dataset submitter | |
Full Dataset Link List
Dataset FTP location
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PRIDE project URI |
Repository Record List
[ + ]
[ - ]
- PRIDE
- PXD057836
- Label: PRIDE project
- Name: Synthesis and Anti-mycobacterial Activity of Novel Medium-chain β-Lactone Derivatives: A Multi-Target Strategy to combat Mycobacterium abscessus and other Pathogenic Mycobacteria