KEA1-97 is a Thioredoxin-Caspase 3 interaction disruptor. It was found to target lysine 72 of thioredoxin, inhibiting its interactions with caspase 3 and inducing apoptosis without affecting other thioredoxin activity. KEA1-97 induced apoptosis in breast cancer cells and treatment of immune-deficient SCID mice at 5 mg/kg ip impaired breast tumor xenograft growth.
ACS chemical biology, 12(10), 2522-2528 (2017-09-12)
Covalent ligand discovery is a promising strategy to develop small-molecule effectors against therapeutic targets. Recent studies have shown that dichlorotriazines are promising reactive scaffolds that preferentially react with lysines. Here, we have synthesized a series of dichlorotriazine-based covalent ligands and
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