[Inhibition of glutamine synthetase activity by biologically active derivatives of glutamic acid].
The inhibition of activity of glutamine synthetase from Chlorella and porcine brain by 4-hydroxy-D-4-fluoro-D,L- and 4-amino-D,L-glutamic acids diastereoisomers was studied. Each compound was shown to exert the same inhibiting effect on glutamine synthetase from both sources. In case of threo-4-hydroxy-D-glutamic acid the inhibition of the Chlorella enzyme was of a competitive and of a completely mixed type. The enzyme inhibition by 4-fluoro-D, L-glutamic acids seemed to be of a completely non-competitive type. The Ki values for all inhibition reactions were determined. A comparison of biochemical parameters and biological activity revealed that the most effective inhibitors of the enzyme exert a most potent antitumour and antiviral action.
Firsova
N A
NA
Selivanova
K M
KM
Alekseeva
L V
LV
Evstigneeva
Z G
ZG
D000818:Animals; D000970:Antineoplastic Agents; D000998:Antiviral Agents; D001921:Brain / Q000201:enzymology; D002708:Chlorella / Q000201:enzymology; D005974:Glutamate-Ammonia Ligase / Q000037:antagonists & inhibitors*; D005971:Glutamates / Q000494:pharmacology*; D018698:Glutamic Acid; D066298:In Vitro Techniques; D007700:Kinetics; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013552:Swine
D000970:Antineoplastic Agents; D000998:Antiviral Agents; D005971:Glutamates; D018698:Glutamic Acid; D005974:Glutamate-Ammonia Ligase
Ingibirovanie aktivnosti glutaminsintetazy biologicheski aktivnymi proizvodnymi glutaminovoĭ kisloty.