| Autor: |
Schirlin, Daniel, Baltzer, Sylvie, Heydt, Jean-Georges, Jung, Michel |
| Zdroj: |
Journal of Enzyme Inhibition; 1987, Vol. 1 Issue: 4 p243-258, 16p |
| Abstrakt: |
β-Difluoromethyl-β-alanine (3-amino-4,4-difluorobutanoic acid) is a potent in vitro and in vivo inhibitor of GABA-T. The rate of inhibition of GABA-T is concentration- and time-dependent. The inactivation is active-site directed. No reactive species escapes from the active site before reacting with the enzyme. The inhibition is irreversible and stereospecific. The use of β-2H-β-difluoromethyl-β-alanine results in a marked primary isotope effect in vitro and in vivo. The use of differently substituted dihalogeno derivatives of β-alanine suggests that the rate of inhibition is dependent on the nature and position of the leaving group. The mechanism of inhibition is discussed on the basis of spectral changes. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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