Formation of [Leu5]Enkephalin from Dynorphin A(1?8) by Rat Central Nervous Tissue In Vitro
- 31 March 1990
- journal article
- research article
- Published by Wiley in Journal of Neurochemistry
- Vol. 54 (4) , 1379-1385
- https://doi.org/10.1111/j.1471-4159.1990.tb01972.x
Abstract
[3H]Dynorphin A(1-8) is readily metabolised by rat lumbosacral spinal cord tissue in vitro, affording a variety of products including a significant amount (20% recovered activity) of [3H]Leu5]enkephalin. In the presence of the peptidase inhibitors bestatin, captopril, thiorphan, and leucylleucine, [3H][Leu5]enkephalin was the major metabolic product, accounting for 60% of recovered activity. Production of [3H][Leu5]enkephalin was seen across all gross brain regions. The enzyme responsible for the cleavage has an optimal substrate length of 8-13 amino acids and is inhibited by N-[1-(RS)-carboxy-2-phenylethyl]-Ala-Ala-Phe-p-aminobenzoate, a site-directed inhibitor of the metalloendopeptidase EC 3.4.24.15. However the enzymic breakdown also has properties in common with involvement of endo-oligopeptidase A. Possible consequences of the formation of [Leu5]-enkephalin from the smaller dynorphins are discussed.Keywords
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