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Literature summary for 2.7.1.48 extracted from

  • Sarkisjan, D.; Julsing, J.R.; Smid, K.; de Klerk, D.; van Kuilenburg, A.B.; Meinsma, R.; Lee, Y.B.; Kim, D.J.; Peters, G.J.
    The cytidine analog fluorocyclopentenylcytosine (RX-3117) is activated by uridine-cytidine kinase 2 (2016), PLoS ONE, 11, e0162901 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.1.48

Application

Application Comment Organism
drug development RX-3117, an orally available cytidine analogue, is activated by UCK2 which may be used to select patients potentially sensitive to RX-3117 Homo sapiens

Protein Variants

Protein Variants Comment Organism
additional information enzyme silencing by transfection of A549 and SW1573 cell lines with UCK-siRNAs. Transfection of UCK1-siRNA efficiently downregulates UCK1-mRNA, but not UCK2-mRNA expression, and does not affect sensitivity to RX-3117. Transfection of UCK2-siRNA completely downregulates UCK2-mRNA and protein and protects both A549 and SW1573 against RX-3117 Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + cytidine Homo sapiens
-
 ADP + CMP
-
 ?
ATP + uridine Homo sapiens
-
 ADP + UMP
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9BZX2
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-549 cell
-
 Homo sapiens
-
additional information enzyme activity in two panels of tumor cell lines and xenograft cells correlated only with UCK2-mRNA expression, but not with UCK1-mRNA. Moreover, accumulation of RX-3117 nucleotides correlates with UCK2 expression Homo sapiens
-
SW-1573 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + 4-amino-1-[(1S,4R,5S)-2-fluoro-4,5-dihydroxy-3-(hydroxymethyl)cyclopent-2-en-1-yl]pyrimidin-2(1H)-one
-
 Homo sapiens ADP + [(3S,4S,5R)-3-(4-amino-2-oxopyrimidin-1(2H)-yl)-2-fluoro-4,5-dihydroxycyclopent-1-en-1-yl]methyl phosphate
-
 ir
ATP + cytidine
-
 Homo sapiens ADP + CMP
-
 ?
ATP + fluorocyclopentenylcytosine an orally available cytidine analogue, RX-3117 Homo sapiens ?
-
 ?
ATP + uridine
-
 Homo sapiens ADP + UMP
-
 ?

Synonyms

Synonyms Comment Organism
uridine-cytidine kinase 2
-
 Homo sapiens

General Information

General Information Comment Organism
physiological function enzyme activity in two panels of tumor cell lines and xenograft cells correlated only with UCK2-mRNA expression, but not with UCK1-mRNA. Moreover, accumulation of RX-3117 nucleotides correlates with UCK2 expression Homo sapiens