Amino acids and peptides .44. Synthesis of stereoisomeric pentapeptides of thiol proteinase inhibitor

被引:0
|
作者
Iguchi, S
Hirano, K
Okamoto, H
Okamoto, Y
Okada, Y
机构
[1] KOBE GAKUIN UNIV, FAC PHARMACEUT SCI, NISHI KU, KOBE 65121, JAPAN
[2] DAIICHI COLL PHARMACEUT SCI, MINAMI KU, FUKUOKA 815, JAPAN
关键词
thiol proteinase inhibitor; TPI common sequence; stereoisomeric pentapeptide; structure-activity relationship; circular dichroism spectra;
D O I
暂无
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Stereoisomers of thiol proteinase inhibitor (TPI) were synthesized by a conventional solution method, Among them, iNoc-D-Gln-Val-Val-Ala-Ala-pNA weakly inhibited the amidolytic activity of papain, although iNoc-Gln-Val-Val-Ala-Ala-pNA inhibited papain activity fairly potently, However, the other five D-amino acid-containing peptides did not show any inhibitory effects on papain. The circular dichroism (CD) spectra of the enzyme-peptides mixtures were measured in order to study the relationship between the peptide anilides-papain interaction and the inhibitory activity.
引用
收藏
页码:1599 / 1602
页数:4
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