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

  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},
  volume={28 11},
  • W. Shen, H. Ryser
  • Published 16 March 1981
  • Biology, Chemistry, Materials Science
  • Life sciences
Methotrexate conjugate with branched polypeptide influences Leishmania donovani infection in vitro and in experimental animals.
It is demonstrated that MTX conjugates in which the drug is covalently attached to carrier have pronounced leishmanicid activity, and the number of Leishmania donovani parasites in infected macrophages are markedly reduced in conjugate treated animals.
Drug-Poly(Lysine) Conjugates: Their Potential for Chemotherapy and for the Study of Endocytosis
The membrane transport of poly(Lys), a strongly cationic macromolecule, can be defined as non-specific adsorptive endocytosis, as opposed to fluid-phase endocydosis or to receptor-mediated endocyTosis.
Targeting, internalization, and cytotoxicity of methotrexate-monoclonal anti-stage-specific embryonic antigen-1 antibody conjugates in cultured F-9 teratocarcinoma cells.
Results indicate that the MTX antibody conjugate binds specifically to F-9 cells, and is internalized and intracellularly degraded to release a small molecular active drug.
Drug Delivery with Protein and Peptide Carriers
The mechanism by which the drug is taken up into a cellular target may be altered for the drug-carrier complex and, in the case of an antibody carrier, tissue specificity may also be added to the properties of the drug.


Poly (L-lysine) and poly (D-lysine) conjugates of methotrexate: different inhibitory effect on drug resistant cells.
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.
Photoinactivation of the methotrexate transport system of L1210 cells by 8-azidoadenosin 5'-monophosphate.
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.