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We report herein a set of activity-based probes (ABPs; P3-P7) based on various lysine-reactive covalent warheads capable of global profiling of ligandable lysine within BRDs in live cells and animals. Chemoproteomic experiments with P7 by utilizing 2-ethynylbenzaldehyde (EBA) identified 18 endogenou...
ORGANISM(S): Homo Sapiens Mus Musculus 
Recent advances in chemical proteomics have begun to characterize the reactivity and ligandability of lysines on a global scale. Yet, only a limited diversity of aminophilic electrophiles have been evaluated for interactions with the lysine proteome. Here, we report an in-depth profiling of >30 unch...
ORGANISM(S): Homo sapiens (Human) 
2021-09-20 | PXD025829 | Pride
The development of various heteroaromatic activated esters designed for selective lysine labeling within the proteome for profiling purposes. Through systematic optimization of the reactivity and selectivity of these esters, we identified a series of effective probe molecules suitable for both in vi...
ORGANISM(S): Homo Sapiens 
Suzuki-Miyauara cross-coupling has been used for mass-spectrometry-based chemoproteomics, including for target deconvolution and site of labeling studies. We also demonstrated that Suzuki-Miyauara cross coupling and CuAAC can be combined for dual target labeling for mass spectrometry-based proteomic...
ORGANISM(S): Homo sapiens (Human) 
2021-02-03 | PXD022279 | Pride
Bromodomain (BRD) is an epigenetic reader of acetylated lysine. It has emerged as a therapeutic target for cancer and other diseases. Current nonselective BRD inhibitors (BRDis) face several adverse events (i.e. gastrointestinal toxicity and thrombocytopenia), making the development of target covale...
ORGANISM(S): Homo sapiens 
2024-12-11 | GSE283487 | GEO
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