Synthesis of Enkephalin Aminopeptidase Inhibitors

엔케파린 아미노펩티다제 저해물 합성

  • Moon Byung Jo (College of Natural Sciences, Kyungpook National University) ;
  • Cha, Jong Won (College of Natural Sciences, Kyungpook National University) ;
  • Kwon Oh Shin (College of Natural Sciences, Kyungpook National University)
  • 문병조 (경북대학교 자연과학대학 생화학과) ;
  • 차종원 (경북대학교 자연과학대학 생화학과) ;
  • 권오신 (경북대학교 자연과학대학 생화학과)
  • Published : 1991.02.20

Abstract

In an effort to increase effective action of enkephalins, several peptide inhibitors of enkephalin aminopeptidase have been synthesized. The peptides contain 3-amino-2-hydroxy amino acid as a zinc binding site and side chains of substrate pattern. The peptides were synthesized in solution by chain elongation from C-terminal end using DCC/HOBt as coupling reagent. The peptides are shown to have very strong inhibitory activity against enkephalin aminopeptidase.

Enkephalin의 작용을 연장하기 위한 연구이 하나로서 수개의 enkephalin aminopeptidase의 저해물을 합성하였다. 이 펩티드성 저해물은 zinc 결합자리로서 3-amino-2-hydroxy amino acid와 기질양상의 곁사슬을 가진다. 펩티드들은 용액 중에서 DCC/HOBt를 축합시약으로 사용하여 C-말단으로부터 사슬 연장법으로 합성하였다. 합성한 펩티드 저해물들은 모두 enkephalin aminopeptidase에 대하여 강한 저해 작용을 나타내었다.

Keywords

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