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PXD039931-2

PXD039931 is an original dataset announced via ProteomeXchange.

Dataset Summary
TitleSolid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows
DescriptionMacrocyclic peptides are attractive for chemoproteomic applications due to their modular synthesis and potential for high target selectivity. We describe a solid phase synthesis method for the efficient generation of libraries of small macrocycles that contain an electrophile and alkyne handle. The modular synthesis produces libraries that can be directly screened using simple SDS-PAGE readouts and then optimal lead molecules applied to proteomic analysis. We generated a library of 480 macrocyclic peptides containing the weakly reactive fluorosulfate (OSF) electrophile. Initial screening of a subset of the library containing each of the various diversity elements identified initial molecules of interest. The corresponding positional and confirmational isomers were then screened to select molecules that showed specific protein labeling patterns that were dependent on the probe structure. The most promising hits were applied to standard chemoproteomic workflows to identify protein targets. Our results demonstrate the feasibility of rapid, on-resin synthesis of diverse macrocyclic electrophiles to generate new classes of covalent ligands.
HostingRepositoryPRIDE
AnnounceDate2023-11-14
AnnouncementXMLSubmission_2023-11-14_08:24:27.204.xml
DigitalObjectIdentifier
ReviewLevelPeer-reviewed dataset
DatasetOriginOriginal dataset
RepositorySupportUnsupported dataset by repository
PrimarySubmitterDaniel Abegg
SpeciesList scientific name: Homo sapiens (Human); NCBI TaxID: 9606;
ModificationListmonohydroxylated residue; iodoacetamide derivatized residue
InstrumentQ Exactive HF-X
Dataset History
RevisionDatetimeStatusChangeLog Entry
02023-02-07 14:28:21ID requested
12023-03-02 16:11:57announced
22023-11-14 08:24:27announced2023-11-14: Updated project metadata.
Publication List
Dataset with its publication pending
Keyword List
submitter keyword: SuFEx, chemoproteomics, electrophile, macrocycles,Fluorosulfate
Contact List
Dr. Alexander Adibekian
contact affiliationDepartment of Chemistry University of Illinois at Chicago 845 West Taylor Street - Room 1454 SES Chicago, Illinois, 60607, USA
contact emailaadibeki@uic.edu
lab head
Daniel Abegg
contact affiliationUniversity of Illinois at Chicago
contact emaildabegg@uic.edu
dataset submitter
Full Dataset Link List
Dataset FTP location
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PRIDE project URI
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