PXD038375 is an
original dataset announced via ProteomeXchange.
Dataset Summary
Title | Sulfamate acetamides as self-immolative electrophiles for covalent ligand- directed release chemistry - Pull Down data |
Description | Electrophiles for covalent inhibitors that are suitable for in vivo administration are rare. While acrylamides are prevalent in FDA approved covalent drugs, chloroacetamides are considered too reactive for such purposes. We report sulfamate-based electrophiles that maintain chloroacetamide-like geometry, with tunable reactivity. We prepared sulfamate-based inhibitors for BTK and Pin1 displaying high potency, low intrinsic reactivity and high stability. Finally, we show that sulfamate acetamides can be used for covalent ligand-directed release (CoLDR) chemistry, both for the generation of ‘turn-on’ probes as well as for traceless ligand-directed site-specific labeling of proteins. Using alkyne-modified sulfamate-based probes, we performed proteomics studies with samples enriched with probe-bound proteins, and the sulfamate probes displayed comparable or improved selectivity compared to the parent compounds. Further characterization of off-target using IsoDTB-ABPP confirmed this result. This submission contains the pull down data. |
HostingRepository | PRIDE |
AnnounceDate | 2023-11-14 |
AnnouncementXML | Submission_2023-11-14_08:44:01.517.xml |
DigitalObjectIdentifier | https://dx.doi.org/10.6019/PXD038375 |
ReviewLevel | Peer-reviewed dataset |
DatasetOrigin | Original dataset |
RepositorySupport | Supported dataset by repository |
PrimarySubmitter | Ronen Gabizon |
SpeciesList | scientific name: Homo sapiens (Human); NCBI TaxID: 9606; |
ModificationList | acetylated residue; monohydroxylated residue; iodoacetamide derivatized residue |
Instrument | Orbitrap Exploris 240 |
Dataset History
Revision | Datetime | Status | ChangeLog Entry |
0 | 2022-11-26 03:38:59 | ID requested | |
1 | 2023-03-11 11:16:47 | announced | |
⏵ 2 | 2023-11-14 08:44:08 | announced | 2023-11-14: Updated project metadata. |
Publication List
10.6019/PXD038375; |
Reddi RN, Rogel A, Gabizon R, Rawale DG, Harish B, Marom S, Tivon B, Arbel YS, Gurwicz N, Oren R, David K, Liu J, Duberstein S, Itkin M, Malitsky S, Barr H, Katz BZ, Herishanu Y, Shachar I, Shulman Z, London N, Sulfamate Acetamides as Self-Immolative Electrophiles for Covalent Ligand-Directed Release Chemistry. J Am Chem Soc, 145(6):3346-3360(2023) [pubmed] |
Keyword List
submitter keyword: Human, Pull down, Chemical Probes |
Contact List
Nir London |
contact affiliation | Department of Chemical and Structural Biology, Weizmann Institute of Science, Rehovot 76100, Israel |
contact email | Nir.London@weizmann.ac.il |
lab head | |
Ronen Gabizon |
contact affiliation | Department of Chemical and Structural Biology, Weizmann Institute of Science |
contact email | ronen.gabizon@weizmann.ac.il |
dataset submitter | |
Full Dataset Link List
Dataset FTP location
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PRIDE project URI |
Repository Record List
[ + ]
[ - ]
- PRIDE
- PXD038375
- Label: PRIDE project
- Name: Sulfamate acetamides as self-immolative electrophiles for covalent ligand- directed release chemistry - Pull Down data