| Autor: |
Vasyutina, E., Bugreev, D., Ryabinin, V., Sinyakov, A., Buneva, V., Nevinskii, G. |
| Zdroj: |
Molecular Biology; May2000, Vol. 34 Issue 3, p356-362, 7p |
| Abstrakt: |
Nonnatural thiazole-containing oligopeptides (TCOs) bind to the DNA minor groove and inhibit the reaction catalyzed by human topoisomerase I (TopoI). The effect is directly proportional to the number of thiazole monomers in TCO. Several TCOs with three or four thiazole monomers act 3–10 times more efficiently than distamycin A, a natural antibiotic containing pyrrole rings. Additional groups at the N and C termini only slightly affect TopoI inhibition by TCO. The inhibitory effect of TCOs is higher than that of homo-or heterooligopeptides containing imidazole or pyrrole monomers, and the most potent are oligopeptide-oligonucleotide conjugates. The plausible causes of the different effects of distamycin and the nonnatural peptides on DNA relaxation catalyzed by TopoI are discussed. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
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