TMC-95A, B, C, and D, novel proteasome inhibitors produced by Apiospora montagnei Sacc. TC 1093 -: Taxonomy, production, isolation, and biological activities

被引：245

作者：

Koguchi, Y ^{[1
]}

Kohno, J ^{[1
]}

Nishio, M ^{[1
]}

Takahashi, K ^{[1
]}

Okuda, T ^{[1
]}

Ohnuki, T ^{[1
]}

Komatsubara, S ^{[1
]}

机构：

[1] Tanabe Seiyaku Co Ltd, Dept Basic Technol, Discovery Res Lab, Toda, Saitama 3358505, Japan

来源：

JOURNAL OF ANTIBIOTICS | 2000年 / 53卷 / 02期

关键词：

D O I：

10.7164/antibiotics.53.105

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

In our course of screening for novel proteasome inhibitors, TMC-95A and its diastereomers, TMC-95B to D, were isolated from the fermentation broth of Apiospora montagnei Sacc. TC 1093. TMC-95A inhibited the chymotrypsin-like (ChT-L), trypsin-like (TL), and peptidylglutamyl-peptide hydrolyzing (PGPH) activities of 20S proteasome with IC50 values of 5.4nM, 200 nM, and 60 nM, respectively. TMC-95B inhibited these activities to the same extent as TMC-95A, while the inhibitory activities of TMC-95C and D were 20 to 150 times weaker than that of TMC-95A and B. TMC-95A did not inhibit m-calpain, cathepsin L, and trypsin at 30 mu M, suggesting its high selectivity for proteasome. Taxonomy of the producing strain is also described.

引用

页码：105 / 109

页数：5

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