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Amino acids and peptides. XXXVI. Synthesis of enkephalin chloromethyl ketone and evaluation of its inhibitory activity against endopeptidase 22.19
Authors:H Taguchi  Y Nishiyama  AC Camargo  Y Okada
Affiliation:Faculty of Pharmaceutical Sciences, Kobe-Gakuin University, Japan.
Abstract:Boc-Tyr-Gly-Gly-Phe-Leu-Ch2Cl was synthesized by the conventional solution method. During the course of acid hydrolysis (6N HCl, 110 degrees C, 18h) of Boc-Phe-Leu-CH2Cl, side reaction occurred, resulting in low recovery of Phe residue on amino acid analysis. The inhibitory activity of the synthesized Boc-Tyr-Gly-Gly-Phe-Leu-CH2Cl against endopeptidase 22.19, an enzyme related to the metabolism of opioid peptides, was examined.
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