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Updated: Apr 4, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Inhibitors of BCATm: A Tough Nut To Crack
1Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University , Parkville, Victoria 3052, Australia.
Abstract:
Inhibitors of the mitochondrial branched chain aminotransferase may have therapeutic potential in the treatment of diet-induced obesity and dyslipidemia. To explore the pharmacology of this metabolic pathway requires a potent and selective molecule that is well tolerated and has appropriate pharmacokinetic properties. The combination of fragment-based and high-throughput screening with structure-guided compound elaboration has yielded a tool compound that may serve as a chemical probe of this pathway.
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