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ProteomicsSulfamate acetamides as self-immolative electrophiles for covalent ligand- directed release chemistry
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 geom...
ORGANISM(S): Homo sapiens (Human) 
2023-03-11 | PXD038301 | Pride
Human Chemical probes Isodtb 
ProteomicsSulfamate acetamides as self-immolative electrophiles for covalent ligand- directed release chemistry - Pull Down data
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 geom...
ORGANISM(S): Homo sapiens (Human) 
2023-03-11 | PXD038375 | Pride
Human Pull down Chemical probes 
UnknownNext-Generation Heterocyclic Electrophiles as Small-Molecule Covalent MurA Inhibitors.
Not available
S-EPMC9781958 | biostudies-literature
UnknownSulfamate Acetamides as Self-Immolative Electrophiles for Covalent Ligand-Directed Release Chemistry.
Not available
S-EPMC9936582 | biostudies-literature
UnknownCovalent Ligand Electrophiles Are Differentially Activated by Proximity Effects Which Govern Latent Protein Reactivity.
Not available
S-EPMC12550623 | biostudies-literature
ProteomicsProteome-wide profiling of the selectivity of diverse electrophiles
Targeted covalent inhibitors (TCIs) are established as powerful entities in drug discovery, but their application has so far mainly been limited to addressing cysteine. Competitive, residue-specific proteomics has been instrumental to streamline covalent drug discovery targeting cysteine. Several pr...
ORGANISM(S): Homo sapiens (Human) Staphylococcus aureus 
2025-08-09 | PXD024454 | Pride
Covalent inhibitors Chemical proteomics Activity-based protein profiling Isodtb-abpp 
ProteomicsThioamide-warheads with enhanced cysteine reactivity and specificity for targeted covalent inhibitors
Targeted covalent inhibitors (TCIs) form covalent bond with their target that requires tailored reactive functionalities identified as warheads. Here we present a versatile approach changing carboxamide functions with thioamides that transforms known warheads to softer electrophiles enhancing reacti...
ORGANISM(S): Homo sapiens (Human) 
2026-09-07 | PXD054470 | Pride
Warhead Proteomics Cystein Covalent inhibitors 
UnknownSelective covalent targeting of GPX4 using masked nitrile-oxide electrophiles.
Not available
S-EPMC7251976 | biostudies-literature
ProteomicsTopoisomerase I Poisoning by Electrophiles Derived from Oxidative Stress
The cancer target enyzme topoisomerase 1 transiently cleaves one strand of chromosomal DNA to relax accumulated strain that can prevent transcription, replication or chromatin assembly. The topoisomerase 1 poison camptothecin and its synthetic analogs are widely used chemotherapeutics that act by tr...
ORGANISM(S): Homo sapiens (Human) 
2021-03-24 | PXD018549 | Pride
Oxidative stress Chemotherapy Q-exactive Topoisomerases Enzymology Proteomics 
UnknownA Two-Step Synthesis of Covalent Genetically-Encoded Libraries of Peptide-Derived Macrocycles (cGELs) enables use of electrophiles with diverse reactivity.
Not available
S-EPMC12407954 | biostudies-literature
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