Transition-state analogues as inhibitors for GABA-aminotransferase

Magdy Iskander, PR Andrews, David Winkler, RI Brinkworth, C. Di Paola, S. Cavell, J. Issa

Research output: Contribution to journalArticleOther

5 Citations (Scopus)

Abstract

Our previous calculations on the reaction catalysed by GABA-aminotransferase (GABA-T) have been utilized in this work in order to synthesize a series of reversible inhibitors of this enzyme. The synthesized transition-state analogues and their precursors inhibited GABA-T competitively in both the holoenzyme and apoenzyme at 10-3 and 10-5 M, respectively. In the case of the holoenzyme, the transition-state analogue series (the conformationally restricted series) gave a significant increase in inhibition values over the open (less conformationally restricted) series. 

Original languageEnglish
Pages (from-to)129-135
Number of pages7
JournalEuropean Journal of Medicinal Chemistry
Volume26
Issue number2
DOIs
Publication statusPublished - 1991

Keywords

  • biochemical evaluation
  • enzyme inhibitors
  • GABA-aminotransferase
  • transition-state analogues

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