5-氟-2'-脱氧尿苷酸：与胸苷酸合成酶的共价复合物。
5-Fluoro-2'-deoxyuridylate: covalent complex with thymidylate synthetase.
作者信息
Santi D V, McHenry C S
出版信息
Proc Natl Acad Sci U S A. 1972 Jul;69(7):1855-7. doi: 10.1073/pnas.69.7.1855.
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.
摘要
5-氟-2'-脱氧尿苷酸会导致胸苷酸合成酶迅速失活，这种失活依赖于辅因子5,10-亚甲基四氢叶酸的预先络合。酶-5-氟-2'-脱氧尿苷酸复合物可在硝酸纤维素膜上分离得到，且不会被6M尿素破坏。在5,10-亚甲基四氢叶酸存在的情况下，5-氟-2'-脱氧尿苷酸与酶反应时，在269nm处观察到吸光度迅速下降，269nm是嘧啶发色团的最大吸收波长。由此得出结论，5-氟-2'-脱氧尿苷酸的6位与参与催化的酶的亲核基团之间形成了共价键。
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