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Cytostatic Nucleotides

A hallmark of cancer is uncontrolled cell proliferation caused by deregulation of multiple signaling pathways associated with cell replication, metabolism and programmed cell death[1].

Cytostatic nucleotides are substrate analogs of physiological nucleotides that inhibit cell proliferation by interfering with cellular targets involved in DNA/RNA synthesis and nucleotide metabolism.

In vivo or cell culture experiments can be performed using the non-phosphorylated nucleoside variant of a cytostatic nucleotide that is metabolized by multiple cellular kinases to its active phosphorylated forms (NMP → NDP → NTP).

Alternatively, a number of mono-, di- and triphosphorylated analogs of cytostatic nucleotides are available for functional in vitro experiments (Tab. 1).

Please refer to the corresponding data sheet for detailed application data.

Table 1: Available cytostatic nucleosides and corresponding nucleotide variants.

NucleosideNucleotide
Monophosphate (NMP)
Nucleotide
Diphosphate (NDP)
Nucleotide
Triphosphate (NTP)
ara-A
(Vidarabine)
ara-AMP
ara-ATP
Cl-F-ara-A
(Clofarabine)
Cl-F-ara-AMP
Cl-F-ara-ATP
2'Cl-Adenosine

2'Cl-dATP
ara-C
(Cytarabine)
ara-CMPara-CDPara-CTP
dF-dC
(Gemcitabine)
dF-dCMPdF-dCDPdF-dCTP
5F-U
(5-Fluoruracil)
5F-dUMP
5F-dUTP
6-Thio-I
(6-Thio-inosine)
6-Thio-IMP6-Thio-IDP6-Thio-ITP
6-Methylthio-I
(6-Methylthio-inosine)
6-Methylthio-IMP6-Methylthio-IDP6-Methylthio-ITP
5-Aza-dC
(Decitabine)
5-Aza-dCTP

Selected References

[1] Hanahan et al. (2011) Hallmarks of Cancer: The next generation. Cell 144 (5):646.