Inhibitors of BCATm: A Tough Nut To Crack.

J Med Chem

Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.

Published: September 2015

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Article 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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http://dx.doi.org/10.1021/acs.jmedchem.5b01244DOI Listing

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Inhibitors of BCATm: A Tough Nut To Crack.

J Med Chem

September 2015

Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.

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.

View Article and Find Full Text PDF

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