Statins Potentiate Aminopeptidase Inhibitor (Pro) Drug Activity In Acute Myeloid Leukemia Cells

Jacqueline Cloos,Godefridus J Peters,Marjon Al,Yehuda G Assaraf,Lixia Wang,Jack W. Singer,Jorge E. Cortes,Gert J. Ossenkoppele,Gerrit Jansen

BLOOD（2018）

引用 2|浏览14

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摘要

Tosedostat represents a next generation oral aminopeptidase inhibitor prodrug that has recently demonstrated promising activity in elderly patients with relapsed and refractory acute myeloid leukemia (AML). This prodrug is bio-activated to its hydrophilic active metabolite by intracellular esterases including carboxylesterase 1 (CES1) hence enhancing its cellular retention and promoting targeting of multiple aminopeptidases.

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