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In vivo, Ara-C is transported into the cell via the human equilibrium nucleoside transporter (hENT1) and is rapidly phosphorylated by deoxycytidine kinase (dCK) to its monophosphate form, cytosine arabinoside monophosphate (Ara-CMP), which is further phosphorylated by nucleoside kinases and finally to the triphosphorylated and active form, cytosine arabinoside triphosphate (AraCTP).
Gemzar[R] requires the enzyme deoxycytidine kinase (DCK)--manufactured within the cancer cell--to become fully activated.
CYC682 maybe particularly active in tumours with a low ratio of cytidine deaminase to deoxycytidine kinase, two enzymes involved in inactivating and activating respectively the mechanism by which CYC682 acts.
Human Deoxycytidine Kinase 2 WO96/21724 18-Jul-1996 51.