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.
| Nucleoside | Nucleotide 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-CMP | ara-CDP | ara-CTP |
| dF-dC (Gemcitabine) |
dF-dCMP | dF-dCDP | dF-dCTP |
| 5F-U (5-Fluoruracil) |
5F-dUMP | 5F-dUTP | |
| 6-Thio-I (6-Thio-inosine) |
6-Thio-IMP | 6-Thio-IDP | 6-Thio-ITP |
| 6-Methylthio-I (6-Methylthio-inosine) |
6-Methylthio-IMP | 6-Methylthio-IDP | 6-Methylthio-ITP |
| 5-Aza-dC (Decitabine) |
5-Aza-dCTP |
[1] Hanahan et al. (2011) Hallmarks of Cancer: The next generation. Cell 144 (5):646.
