Synthesis, kinetic characterization and X-ray analysis of peptide aldehydes as inhibitors of the 20S proteasomes from Thermoplasma acidophilum and Saccharomyces cerevisiae

被引：2

作者：

Escherich, A ^{[1
]}

Ditzel, L ^{[1
]}

Musiol, HJ ^{[1
]}

Groll, M ^{[1
]}

Huber, R ^{[1
]}

Moroder, L ^{[1
]}

机构：

[1] MAX PLANCK INST BIOCHEM,D-82152 MARTINSRIED,GERMANY

来源：

BIOLOGICAL CHEMISTRY | 1997年 / 378卷 / 08期

关键词：

inhibition; peptide aldehydes; proteasome; X-ray structures;

D O I：

10.1515/bchm.1997.378.8.893

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A comparative kinetic characterization of the peptide aldehydes Ac-Leu-Leu-X-H [X = Trp, Tyr and Tyr(tBu)] and Z-Gly-Pro-Gly-Gly-Leu-Leu-Nle-H as inhibitors of the chymotryptic activity of 20S proteasomes from the archaebacterium T. acidophilum and yeast S. cerevisiae revealed significantly differentiated inhibitory potencies that can be rationalized on the basis of X-ray crystallographic data.

引用

页码：893 / 898

页数：6

共 30 条

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