Effects of a triazine antifolate (NSC 127755) on serine hydroxymethyltransferase in myeloma cells in culture.
The effect of the triazine antifolate NSC 127755 on serine hydroxymethyltransferase activity in mouse myeloma X63 cells in culture was determined. The enzyme was inhibited, apparently irreversibly, with IC50 approximately 5 X 10(-8) M. A similar concentration-dependency for inhibition of [6-3H]deoxyuridine incorporation into DNA was observed in these cells in culture. Long-term culture of myeloma cells with NSC 127755 resulted in a progressive decrease in the number of viable cells. The study emphasises the significance of serine hydroxymethyltransferase as a target for anticancer chemotherapy.
Snell
K
K
Department of Biochemistry, University of Surrey, Guildford, U.K.
Riches
D
D
D000818:Animals; D002470:Cell Survival / Q000187:drug effects; D005493:Folic Acid Antagonists / Q000494:pharmacology*; D012696:Glycine Hydroxymethyltransferase / Q000037:antagonists & inhibitors*; D051379:Mice; D009101:Multiple Myeloma / Q000201:enzymology*; D014166:Transferases / Q000037:antagonists & inhibitors*; D014227:Triazines / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
D005493:Folic Acid Antagonists; D014227:Triazines; C031776:NSC 127755; D014166:Transferases; D012696:Glycine Hydroxymethyltransferase