Selective protection against the cytotoxicity of methotrexate and methotrexate-poly(lysine) by thiamine pyrophosphate, heparin and leucovorin.

@article{Shen1981SelectivePA,
  title={Selective protection against the cytotoxicity of methotrexate and methotrexate-poly(lysine) by thiamine pyrophosphate, heparin and leucovorin.},
  author={Wei Shen and Hugues J.-P. Ryser},
  journal={Life sciences},
  year={1981},
  volume={28 11},
  pages={
          1209-14
        }
}
Abstract The cytotoxicity of both methotrexate (MTX) and methotrexate-poly(L-lysine) conjugate (MTX-poly(lys)) on L929 mouse fibroblasts can be prevented by the simultaneous administration of Leucovorin. Thiamine pyrophosphate, an inhibitor for MTX-transport, protects cells from the toxicity of MTX, but not of MTX-poly(lys). Heparin at low concentration (1 μg/m1) completely abolishes the toxic effect of MTX-poly(lys), but not of MTX. These results suggest that although MTX and MTX-poly(lys… Expand
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References

SHOWING 1-5 OF 5 REFERENCES
Poly (L-lysine) and poly (D-lysine) conjugates of methotrexate: different inhibitory effect on drug resistant cells.
TLDR
Conjugation of methotrexate to poly(L-lysine) markedly increases its cellular uptake and offers a new way to overcome drug resistance related to deficient transport and to give rise in the cell to a pharmacologically active breakdown product. Expand
Photoinactivation of the methotrexate transport system of L1210 cells by 8-azidoadenosin 5'-monophosphate.
TLDR
It is shown that complete photoinactivation of methotrexate transport could not be obtained from a single exposure to 8-azido-AMP, but it could be achieved by the repetitive illumination of cells in a fresh medium and the phosphate and folate/adenine transport systems of L1210 cells are not affected by irradiation in the presence of 7-azidoadenosine-AMP. Expand
Binding properties of the 5-methyltetrahydrofolate/methotrexate transport system in L1210 cells.
TLDR
The measured binding activity does not represent low-temperature transport of substrate into cells, since it is readily saturable with time and is eliminated by either washing the cells with buffer or by the addition of excess unlabeled substrate. Expand
Site of action of a polyanion inhibitor of phagosome-lysosome fusion in cultured macrophages.
TLDR
This semi-synthetic compound chlorite-oxidized amylose (COAM) prepared fromAmylose starch differs from previously reported inhibitors by its rapidity in suppressing P-LF, and shows low toxicity and a wide range of effective dose. Expand
Inhibitory effect of polycations on the transplantability of mouse leukaemia reversed by heparin.
TLDR
L'incubation avec la polyornithine et le Dextran-DEAE, pendant une heure, provoquait une inhibition complete de the transplantabilite, chez 70 a 85% des animaux, and augmentait, de facon significative, the survie des animau restants. Expand