Cytarabine (ara-C) is the most effective chemotherapeutic agent in the treatment of acute myeloid leukemia (AML).
Ara-C is a prodrug that requires extensive intracellular phosphorylation for activation to ara-C 5’triphosphate (ara-CTP).
An uptake transporter known as human equilibrative nucleoside transporter 1 (hENT1) is responsible for ~80% of ara-C uptake into the cell.
Several studies have shown increased hENT1 mRNA expression levels to be correlated with greater chemotherapeutic drug uptake efficacy in multiple patient populations.
Objective: To identify and determine functional and clinical significance of genetic variants in hENT1.
Additional contributors: , Amit K. Mitra; Kristine Crews; Christine Hartford; Stanley Pounds; Xueyuan Cao; Jeffrey Rubnitz; Raul Ribeiro; M. Eileen Dolan; Jatinder K. Lamba (faculty mentor)
This work is supported in part by the National Institutes of Health/National Cancer Institute under grant R01CA132946-01 (Lamba); in part by the Cancer Center Support Grant CA-21765 (St. Jude Children’s Research Hospital); and by the American Lebanese Syrian Associated Charities.
Hart, Michael A..
Identification and Functional Genomic Analysis of Genetic Variants of hENT1.
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