5-Fluoro-2'-deoxyuridylate: covalent complex with thymidylate synthetase.

doi:10.1073/PNAS.69.7.1855

Paper

5-Fluoro-2'-deoxyuridylate: covalent complex with thymidylate synthetase.

Published Jul 1, 1972 · D. Santi, C. McHenry

Proceedings of the National Academy of Sciences of the United States of America

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147

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3

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Abstract

5-Fluoro-2'-deoxyuridylate causes a rapid inactivation of thymidylate synthetase that is dependent upon prior complexation of the cofactor 5,10-methylenetetrahydrofolate. The enzyme-5-fluoro-2'-deoxyuridylate complex may be isolated on nitrocellulose membranes and is not disrupted by 6 M urea. Upon reaction of 5-fluoro-2'-deoxyuridylate with the enzyme in the presence of 5,10-methylenetetrahydrofolate a rapid loss of absorbance is observed at 269 nm, the absorption maximum for the pyrimidine chromophore. It is concluded that a covalent bond is formed between the 6-position of 5-fluoro-2'-deoxyuridylate and a nucleophilic group of the enzyme that is involved in catalysis.

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Study Snapshot

5-Fluoro-2'-deoxyuridylate rapidly inactivates thymidylate synthetase by forming a covalent bond with an enzyme nucleophilic group, causing rapid loss of absorbance at 269 nm.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

5-Fluoro-2'-deoxyuridylate: covalent complex with thymidylate synthetase.

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