Lysine-targeting, covalent inhibitors of bromodomain BD1 of BET proteins in live cells and animals

ABSTRACT: 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 endogenous BRDs, thus giving a global landscape of ligandable lysines in BRDs.

ORGANISM(S): Homo Sapiens Mus Musculus

SUBMITTER: Yusheng Xie  

PROVIDER: PXD058513 | iProX | Thu Apr 10 00:00:00 BST 2025

REPOSITORIES: iProX