- Synthesis and evaluation of novel aromatic substrates and competitive inhibitors of GABA aminotransferase
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The design, synthesis, and evaluation of novel γ-aminobutyric acid aminotransferase (GABA-AT) inhibitors and inactivators can lead to the discovery of new GABA-related therapeutics. To this end, a series of aromatic amino acid compounds was synthesized to aid in the design of new inhibitors and inactivators of GABA-AT. All compounds were tested as competitive inhibitors of GABA-AT. The amino acids with benzylic amines were also tested as substrates for GABA-AT. It was found that these compounds were all poor competitive inhibitors of GABA-AT, but some were substrates of the enzyme, suggesting their utility as scaffolds for potential GABA-AT mechanism-based inactivators. Computer modeling was used to rationalize the substrate activity of the various compounds.
- Clift, Michael D.,Silverman, Richard B.
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p. 3122 - 3125
(2008/12/22)
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- Synthesis of m-Aminomethylbenzoic Acid Peptides
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Several peptides incorporating m-aminomethylbenzoic acid have been synthesized.This amino acid is a conformationally rigid model of a trans dipeptide unit.The products include an analogue of leucine-enkephalin.
- Stewart, Frederick H. C.
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p. 2511 - 2516
(2007/10/02)
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