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

[11] POTENT INHIBITORS OF PROTEASOME
IQBAL, M
CHATTERJEE, S
KAUER, JC
DAS, M
MESSINA, P
FREED, B
BIAZZO, W
SIMAN, R
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1995, 38 (13) : 2276 - 2277
[12] ITO A, 1975, CHEM PHARM BULL, V23, P3106
[13] ITO A, 1975, CHEM PHARM BULL, V23, P3081
[14] CRYSTAL-STRUCTURE OF THE 20S PROTEASOME FROM THE ARCHAEON T-ACIDOPHILUM AT 3.4-ANGSTROM RESOLUTION
LOWE, J
STOCK, D
JAP, R
ZWICKL, P
BAUMEISTER, W
HUBER, R
[J]. SCIENCE, 1995, 268 (5210) : 533 - 539
[15] NAHM S, 1981, TETRAHEDRON LETT, V22, P3812
[16] THE MULTICATALYTIC PROTEINASE COMPLEX, A MAJOR EXTRALYSOSOMAL PROTEOLYTIC SYSTEM
ORLOWSKI, M
[J]. BIOCHEMISTRY, 1990, 29 (45) : 10289 - 10297
[17] EVIDENCE FOR THE PRESENCE OF 5 DISTINCT PROTEOLYTIC COMPONENTS IN THE PITUITARY MULTICATALYTIC PROTEINASE COMPLEX - PROPERTIES OF 2 COMPONENTS CLEAVING BONDS ON THE CARBOXYL SIDE OF BRANCHED-CHAIN AND SMALL NEUTRAL AMINO-ACIDS
ORLOWSKI, M
CARDOZO, C
MICHAUD, C
[J]. BIOCHEMISTRY, 1993, 32 (06) : 1563 - 1572
[18] THE MULTICATALYTIC PROTEINASE OF MAMMALIAN-CELLS
RIVETT, AJ
[J]. ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS, 1989, 268 (01) : 1 - 8
[19] RIVETT AJ, 1993, BIOCHEM J, V291, P1
[20] INHIBITORS OF THE PROTEASOME BLOCK THE DEGRADATION OF MOST CELL-PROTEINS AND THE GENERATION OF PEPTIDES PRESENTED ON MHC CLASS-I MOLECULES
ROCK, KL
GRAMM, C
ROTHSTEIN, L
CLARK, K
STEIN, R
DICK, L
HWANG, D
GOLDBERG, AL
[J]. CELL, 1994, 78 (05) : 761 - 771

← 1 2 3 →