PXD015104 is an
original dataset announced via ProteomeXchange.
Dataset Summary
Title | Expedited mapping of the ligandable proteome using fully functionalized enantiomeric probe pairs |
Description | A fundamental challenge in chemical biology and medicine is to understand and expand the fraction of the human proteome that can be targeted by small molecules. We recently described a strategy that integrates fragment-based ligand discovery with chemical proteomics to furnish global portraits of reversible small molecule-protein interactions in human cells. Excavating clear structure-activity relationships from these “ligandability” maps, however, was confounded by the distinct physicochemical properties and corresponding overall protein-binding potential of individual fragments. Here, we describe a compelling solution to this problem by introducing a next-generation set of fully functionalized fragments (FFFs) differing only in absolute stereochemistry. Using these enantiomeric probe pairs, or “enantioprobes”, we identify numerous stereoselective protein-fragment interactions in cells and show that these interactions occur at functional sites on proteins from diverse classes. Our findings thus indicate that incorporating chirality into FFF libraries provides a robust and streamlined method to discover ligandable proteins in cells. |
HostingRepository | PRIDE |
AnnounceDate | 2024-10-22 |
AnnouncementXML | Submission_2024-10-22_04:57:26.815.xml |
DigitalObjectIdentifier | |
ReviewLevel | Peer-reviewed dataset |
DatasetOrigin | Original dataset |
RepositorySupport | Unsupported dataset by repository |
PrimarySubmitter | Yujia Wang |
SpeciesList | scientific name: Homo sapiens (Human); NCBI TaxID: 9606; |
ModificationList | monohydroxylated residue; iodoacetamide derivatized residue |
Instrument | LTQ Orbitrap Velos; Orbitrap Fusion; LTQ Orbitrap Elite |
Dataset History
Revision | Datetime | Status | ChangeLog Entry |
0 | 2019-08-21 01:01:41 | ID requested | |
1 | 2019-10-29 04:56:03 | announced | |
2 | 2019-11-08 00:39:53 | announced | 2019-11-08: Updated publication reference for PubMed record(s): 31659311. |
⏵ 3 | 2024-10-22 04:57:29 | announced | 2024-10-22: Updated project metadata. |
Publication List
Wang Y, Dix MM, Bianco G, Remsberg JR, Lee HY, Kalocsay M, Gygi SP, Forli S, Vite G, Lawrence RM, Parker CG, Cravatt BF, Expedited mapping of the ligandable proteome using fully functionalized enantiomeric probe pairs. Nat Chem, 11(12):1113-1123(2019) [pubmed] |
10.1038/s41557-019-0351-5; |
Keyword List
submitter keyword: Human, PBMCs, HEK293T, LC-MS/MS |
Contact List
Benjamin F. Cravatt |
contact affiliation | Department of Chemistry The Scripps Research Institute |
contact email | cravatt@scripps.edu |
lab head | |
Yujia Wang |
contact affiliation | The Scripps Research Institute |
contact email | yujia@scripps.edu |
dataset submitter | |
Full Dataset Link List
Dataset FTP location
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PRIDE project URI |
Repository Record List
[ + ]
[ - ]
- PRIDE
- PXD015104
- Label: PRIDE project
- Name: Expedited mapping of the ligandable proteome using fully functionalized enantiomeric probe pairs