A COMPARISON BETWEEN THE BINDING MODES OF A SUBSTRATE AND INHIBITOR TO PAPAIN AS OBSERVED IN COMPLEX CRYSTAL-STRUCTURES

被引：12

作者：

YAMAMOTO, D ^{[1
]}

ISHIDA, T ^{[1
]}

INOUE, M ^{[1
]}

机构：

[1] OSAKA UNIV PHARMACEUT SCI,DEPT PHYS CHEM,2-10-65 KAWAI,MATSUBARA,OSAKA 580,JAPAN

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1990年 / 171卷 / 02期

关键词：

D O I：

10.1016/0006-291X(90)91204-6

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：

On the basis of the crystal structures of papain complexed with the substrate analogue benzyloxycarbonyl-L-phenylalanyl-L-alanine chloromethylketone (Drenth, J., Kalk, K.H., and Swen, H.M. (1976) Biochemistry 15, 3731-3738) and with the inhibitor E-64-c, the binding modes were compared at the atomic level to clarify the functional difference between the substrate and inhibitor. Irrespective of the reverse chemical bonding in the peptide bonds, both the molecules are located at the S subsites of papain with similar interactions. However, the inhibitory activity of E-64-c is characterized by the stereochemical function of a carboxyoxirane ring and the tight binding of the isopentylaminoleucyl side chain to the S subsites. © 1990.

引用

页码：711 / 716

页数：6

共 18 条

[1]

Barrett A.J., 1997, PROTEINASES MAMMALIA, P240

[2] L-TRANS-EPOXYSUCCINYL-LEUCYLAMIDO(4-GUANIDINO)BUTANE (E-64) AND ITS ANALOGS AS INHIBITORS OF CYSTEINE PROTEINASES INCLUDING CATHEPSINS B, H AND L [J].

BARRETT, AJ ;

KEMBHAVI, AA ;

BROWN, MA ;

KIRSCHKE, H ;

KNIGHT, CG ;

TAMAI, M ;

HANADA, K .

BIOCHEMICAL JOURNAL, 1982, 201 (01) :189-198

[3]

BERLIN RD, 1978, MOL BASIS BIOL DEGEN

[4] BINDING OF CHLOROMETHYL KETONE SUBSTRATE ANALOGS TO CRYSTALLINE PAPAIN [J].

DRENTH, J ;

KALK, KH ;

SWEN, HM .

BIOCHEMISTRY, 1976, 15 (17) :3731-3738

[5] STRUCTURE AND SYNTHESIS OF E-64, A NEW THIOL PROTEASE INHIBITOR [J].

HANADA, K ;

TAMAI, M ;

OHMURA, S ;

SAWADA, J ;

SEKI, T ;

TANAKA, I .

AGRICULTURAL AND BIOLOGICAL CHEMISTRY, 1978, 42 (03) :529-536

[6] ISOLATION AND CHARACTERIZATION OF E-64, A NEW THIOL PROTEASE INHIBITOR [J].

HANADA, K ;

TAMAI, M ;

YAMAGISHI, M ;

OHMURA, S ;

SAWADA, J ;

TANAKA, I .

AGRICULTURAL AND BIOLOGICAL CHEMISTRY, 1978, 42 (03) :523-528

[7]

HANADA K, 1983, PROTEINASE INHIBITOR, P23

[8]

Hendrickson WA, 1981, BIOMOLECULAR STRUCTU, V1, P43

[9] MODE OF BINDING OF E-64-C, A POTENT THIOL PROTEASE INHIBITOR, TO PAPAIN AS DETERMINED BY X-RAY CRYSTAL ANALYSIS OF THE COMPLEX [J].

MATSUMOTO, K ;

YAMAMOTO, D ;

OHISHI, H ;

TOMOO, K ;

ISHIDA, T ;

INOUE, M ;

SADATOME, T ;

KITAMURA, K ;

MIZUNO, H .

FEBS LETTERS, 1989, 245 (1-2) :177-180

[10]

Pflugrath J. W., 1984, Methods and Applications in Crystallographic Computing. International Summer School on Crystallographic Computing, P404

← 1 2 →