Autor: |
Licato NJ; Department of Medicinal Chemistry, University of Michigan, Ann Arbor 48109., Coward JK, Nimec Z, Galivan J, Bolanowska WE, McGuire JJ |
Jazyk: |
angličtina |
Zdroj: |
Journal of medicinal chemistry [J Med Chem] 1990 Mar; Vol. 33 (3), pp. 1022-7. |
DOI: |
10.1021/jm00165a021 |
Abstrakt: |
N-[N-(4-Deoxy-4-amino-10-methylpteroyl)-4-fluoroglutamyl]-ga mma-glutamate has been synthesized and its ability to serve as a substrate for folylpolyglutamate synthetase and gamma-glutamyl hydrolase has been investigated. It was anticipated that this compound would be a substrate for both of these enzymes. Although the title compound proved to be a good substrate for folylpolyglutamate synthetase, hydrolysis catalyzed by gamma-glutamyl hydrolase was unexpectedly slow. These results suggest the use of fluoroglutamate-containing peptides as hydrolase-resistant folates or antifols in a variety of chemotherapeutic regimens. |
Databáze: |
MEDLINE |
Externí odkaz: |
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