Inhibitors of BCATm: A Tough Nut To Crack.
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.
Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University , Parkville, Victoria 3052, Australia.
Martin
M
Scanlon
D000818:Animals; D006801:Humans; D024101:Mitochondrial Proteins / Q000037:antagonists & inhibitors*; D011720:Pyrazoles / Q000737:chemistry*; D011744:Pyrimidinones / Q000737:chemistry*; D000637:Transaminases / Q000037:antagonists & inhibitors*
D024101:Mitochondrial Proteins; D011720:Pyrazoles; D011744:Pyrimidinones; D000637:Transaminases