Directory → Antineoplastic funds → Antimetabolita
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The groupAntimetabolitami substances as close to the chemical structure of the endogenous products metabolism and ingibirute making and physiological activity of these metabolites.
Protivoopujolevu activity antimetabolitov discovered in the early 1960s. It was found that methotrexate, a antimetabolitom folic acid is effective in certain tumours rights, especially when horiokartsinome women with acute leukaemia.
By antimetabolitam used as a means of therapy, are structural analogues not only folic acid (methotrexate), but also purinov (mercaptopurine, tioguanin etc.), pirimidinov (ftorurazil, ftorafur, cytarabine). Zitostaticescoe of all of these compounds is in violation of the synthesis of nucleic acids (DNA and RNA). Antagonists folic acid inhibit folatreduktazu restoring folic acid to its active form, tetragidrofolievu acid; Last together with the corresponding transferaza catalyzes the transfer odnouglerodistah fragments in the synthesis of nucleic acids. Analogue purinov violate biosynthesis purinovykh nucleotides. Protivoopujolevoe the pirimidinov of it is transformed into malignant cells in the active inhibitors timidin-sintetaza involved in the synthesis of nucleic acids.