Probing the steric requirements of the γ-aminobutyric acid aminotransferase active site with fluorinated analogues of vigabatrin.

@article{Juncosa2013ProbingTS,
  title={Probing the steric requirements of the γ-aminobutyric acid aminotransferase active site with fluorinated analogues of vigabatrin.},
  author={Jose I. Juncosa and Andrew P Groves and Guoyao Xia and Richard B Silverman},
  journal={Bioorganic & medicinal chemistry},
  year={2013},
  volume={21 4},
  pages={903-11}
}
We have synthesized three analogues of 4-amino-5-fluorohexanoic acids as potential inactivators of γ-aminobutyric acid aminotransferase (GABA-AT), which were designed to combine the potency of their shorter chain analogue, 4-amino-5-fluoropentanoic acid (AFPA), with the greater enzyme selectivity of the antiepileptic vigabatrin (Sabril®). Unexpectedly, these compounds failed to inactivate or inhibit the enzyme, even at high concentrations. On the basis of molecular modeling studies, we propose… CONTINUE READING

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The PyMOL Molecular Graphics System , Version 1 . 4 . 1

K. B. Sharpless, W. Amberg, +6 authors Z. M. Wang
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