Synthesis and interaction with thymidylate synthase of 5'-dithiophosphate and 5'-fluorothiophosphate of thymidine. | Zendy

Barbara Gołos | Zendy; Konrad Misiura | Zendy; Magdalena Olesiak | Zendy; And̀rzej Okruszek | Zendy; Wojciech J. Stec | Zendy; Wojciech Rode | Zendy

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Synthesis and interaction with thymidylate synthase of 5'-dithiophosphate and 5'-fluorothiophosphate of thymidine.

Author(s) -

Barbara Gołos,

Konrad Misiura,

Magdalena Olesiak,

And̀rzej Okruszek,

Wojciech J. Stec,

Wojciech Rode

Publication year - 1998

Publication title -

acta biochimica polonica

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.452

H-Index - 78

eISSN - 1734-154X

pISSN - 0001-527X

DOI - 10.18388/abp.1998_4289

Subject(s) - thymidylate synthase , thymidine , nucleotide , chemistry , enzyme , phosphate , pyrimidine , biochemistry , stereochemistry , thymidine kinase , dna , biology , genetics , chemotherapy , fluorouracil , virus , herpes simplex virus , gene

Thymidine-5'-fluorothiophosphate, dTMP(S)-F, was synthesized by the oxathiaphospholane, and thymidine 5'-dithiophosphate, dTMPS2, by the dithiaphospholane, method. To estimate the role of 5'-phosphate group ionization in binding of pyrimidine nucleotides by thymidylate synthase, dTMP(S)-F was studied as an inhibitor of mouse tumour (L1210) enzyme, and its inhibitory properties were compared with those of dTMPS2, a close dTMP analogue. While dTMPS2 proved to be an inhibitor, competitive vs dUMP, with K(i)app = 94 microM, the 5'-fluorothiophosphate congener displayed no activity, indicating that the enzyme requires for binding the presence of a dianionic 5'-phosphate group in a nucleotide.

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