Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 1.17.4.1 extracted from

  • Saiko, P.; Graser, G.; Giessrigl, B.; Lackner, A.; Grusch, M.; Krupitza, G.; Basu, A.; Sinha, B.; Jayaprakash, V.; Jaeger, W.; Fritzer-Szekeres, M.; Szekeres, T.
    A novel N-hydroxy-N-aminoguanidine derivative inhibits ribonucleotide reductase activity: Effects in human HL-60 promyelocytic leukemia cells and synergism with arabinofuranosylcytosine (Ara-C) (2011), Biochem. Pharmacol., 81, 50-59.
    View publication on PubMed
Search for more literature for 1.17.4.1

Application

Application Comment Organism
medicine combination of (2E)-2-(anthracen-9-ylmethylidene)-N-hydroxyhydrazinecarboximidamide with the first-line antileukemic agent arabinofuranosylcytosine, Ara-C, synergistically potentiates the antineoplastic effects of Ara-C Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2E)-2-(anthracen-9-ylmethylidene)-N-hydroxyhydrazinecarboximidamide i.e. ABNM-13, application leads to significant alterations of deoxyribonucleoside triphosphate pool balance and a highly significant decrease of incorporation of radiolabeled cytidine into DNA of HL-60 cells. Diminished ribonucleotide reductase activity causes replication stress which is consistent with activation of Chk1 and Chk2, resulting in downregulation/degradation of Cdc25A. Cdc25B is upregulated, leading to dephosphorylation and activation of Cdk1. The combined disregulation of Cdc25A and Cdc25B is the most likely cause for ABNM-13 induced S-phase arrest Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HL-60 cell promyelocytic leukemia cell Homo sapiens
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.011
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens (2E)-2-(anthracen-9-ylmethylidene)-N-hydroxyhydrazinecarboximidamide