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Molecular mechanism of thymidylate synthase-catalysed reaction and interaction of the enzyme with 2- and-or 4-substituted analogues of dUMP and 5-fluoro-dUMP

100%

Rode W., Les A.

Acta Biochimica Polonica

1996

tom 43

nr 1

Thymidylate synthase is a target enzyme in anticancer, antiviral, antifungal and antiprotozoan chemotherapy. With two dUMP analogues, 5-fluoro-dUMP (FdUMP) and 5-(trifluoromethyl)-dUMP (CF3dUMP), strong thymidylate synthase inhibitors and active forms of drugs, the inhibition mechanism is based on the reaction mechanism. Recent comparative studies of new dUMP analogues, containing more than one substituent in the pyrimidine ring, showed that substitution of the pyrimidine ring Qd=0 group in FdUMP by either C(4)=N-OH group (in N4-hydroxy-FdCMP) or C(4)=S group (in 4-thio-FdUMP) preserves high inhibitory potency of the drug but may alter its specificity for thymidylate synthases from various sources, which differ in sensitivity to slow-binding inhibition by FdUMP. Informations suggesting mechanisms responsible for the foregoing have been reviewed, including results of molecular modeling studies suggesting interaction of the pyrimidine C(4)=0 group, or its modification, with the N4-methylene-

Topoisomerase II as a target for anticancer chemotherapy

100%

Kaufmann S. H., Hancock R.

Acta Biochimica Polonica

1995

tom 42

nr 4

Type II DNA topoisomerases are required for the segregation of genomic DNA at cell division in prokaryotic and eukaryotic cells, and inhibitors of these enzymes are potential cytotoxic agents in both prokaryotes and eukaryotes. The bacterial member of the topoisomerase II family, DNA gyrase, and the chemotherapeutic agents which target it are the subject of a recent review (Maxwell, A. et al., 1993, in Molecular Biology of DNA Topoisomerases, Andoh, T. et al., eds.,pp. 21-30, CRC Press, Boca Raton). Here we present an overview of current knowledge of eukaryotic topoisomerase II and the anticancer agents which target this enzyme, focussing predominantly on new observations and recent reports and reviews.

Ograniczanie wyników

2 Acta Biochimica Polonica

1 Hancock R.

1 Kaufmann S. H.

1 Les A.

1 Rode W.

1 1996

1 1995

Wyniki wyszukiwania

Molecular mechanism of thymidylate synthase-catalysed reaction and interaction of the enzyme with 2- and-or 4-substituted analogues of dUMP and 5-fluoro-dUMP

Topoisomerase II as a target for anticancer chemotherapy