期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 10, 页码 3122-3125出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.10.060
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资金
- NIGMS NIH HHS [GM66132, R01 GM066132, R01 GM066132-03, R01 GM066132-01A2, R01 GM066132-02, R01 GM066132-04] Funding Source: Medline
The design, synthesis, and evaluation of novel gamma-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. (c) 2007 Elsevier Ltd. All rights reserved.
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