AI Article Synopsis
- γ-Glutamylcyclotransferase (GGCT) is an enzyme that plays a key role in the γ-glutamyl cycle by breaking down γ-glutamyl-amino acids, producing 5-oxoproline and amino acids.
- Eighteen N-acyl-L-alanine analogues were synthesized to test their ability to inhibit GGCT, with Simple N-glutaryl-L-alanine emerging as the most effective inhibitor.
- Analogues with 2-position methyl or dimethyl substitutions showed moderate inhibition, while substrates with specific 3-position modifications exhibited strong inhibitory effects.
Article Abstract
γ-Glutamylcyclotransferase (GGCT) is an important enzyme that cleaves γ-glutamyl-amino acid in the γ-glutamyl cycle to release 5-oxoproline and amino acid. Eighteen N-acyl-L-alanine analogues including eleven new compounds have been synthesized and examined for their inhibitory activity against recombinant human GGCT protein. Simple N-glutaryl-L-alanine was found to be the most potent inhibitor for GGCT. Other N-glutaryl-L-alanine analogues having methyl and dimethyl substituents at the 2-position were moderately effective, while N-(3R-aminoglutary)-L-alanine, the substrate having an (R)-amino group at the 3-position or N-(N-methyl-3-azaglutaryl)-L-alanine, the substrate having an N-methyl substituent on the 3-azaglutaryl carbon, in constract, exhibited excellent inhibition properties.
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| http://dx.doi.org/10.1248/cpb.c16-00167 | DOI Listing |
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