X-RAY CRYSTALLOGRAPHIC STRUCTURE OF A PAPAIN LEUPEPTIN COMPLEX

被引：119

作者：

SCHRODER, E ^{[1
]}

PHILLIPS, C ^{[1
]}

GARMAN, E ^{[1
]}

HARLOS, K ^{[1
]}

CRAWFORD, C ^{[1
]}

机构：

[1] UNIV OXFORD,MOLEC BIOPHYS LAB,REX RICHARDS BLDG,S PARKS RD,OXFORD OX1 3QU,ENGLAND

来源：

FEBS LETTERS | 1993年 / 315卷 / 01期

关键词：

LEUPEPTIN; PAPAIN; ENZYME-INHIBITOR COMPLEX; OXYANION HOLE; HEMITHIOACETAL; X-RAY CRYSTALLOGRAPHY;

D O I：

10.1016/0014-5793(93)81128-M

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：

The three-dimensional structure of the papain-leupeptin complex has been determined by X-ray crystallography to a resolution of 2.1 angstrom (overall R-factor = 19.8%). The structure indicates that: (i) leupeptin contacts the S subsites of the papain active site and not the S' subsites; (ii) the 'carbonyl' carbon atom of the inhibitor is covalently bound by the Cys-25 sulphur atom of papain and is tetrahedrally coordinated; (iii) the 'carbonyl' oxygen atom of the inhibitor faces the oxyanion hole and makes hydrogen bond contacts with Gln-19 and Cys-25.

引用

页码：38 / 42

页数：5

共 30 条

[1] MECHANISM OF ACTION OF PAPAIN WITH A SPECIFIC ANILIDE SUBSTRATE
ANGELIDES, KJ
FINK, AL
[J]. BIOCHEMISTRY, 1979, 18 (11) : 2355 - 2363
[2] MECHANISM OF THIOL PROTEASE CATALYSIS - DETECTION AND STABILIZATION OF A TETRAHEDRAL INTERMEDIATE IN PAPAIN CATALYSIS
ANGELIDES, KJ
FINK, AL
[J]. BIOCHEMISTRY, 1979, 18 (11) : 2363 - 2369
[3] Aoyagi T, 1975, PROTEASES BIOL CONTR, P429
[4] MECHANISM OF ACTION OF CYSTEINE PROTEINASES - OXYANION BINDING-SITE IS NOT ESSENTIAL IN THE HYDROLYSIS OF SPECIFIC SUBSTRATES
ASBOTH, B
STOKUM, E
KHAN, IU
POLGAR, L
[J]. BIOCHEMISTRY, 1985, 24 (03) : 606 - 609
[5] TRANSITION-STATE STABILIZATION AT THE OXYANION BINDING-SITES OF SERINE AND THIOL PROTEINASES - HYDROLYSES OF THIONO AND OXYGEN ESTERS
ASBOTH, B
POLGAR, L
[J]. BIOCHEMISTRY, 1983, 22 (01) : 117 - 122
[6] INHIBITION OF PAPAIN BY N-ACYL-AMINOACETALDEHYDES AND N-ACYL-AMINOPROPANONES - EVIDENCE FOR HEMITHIOACETAL FORMATION BY A CROSS-SATURATION TECHNIQUE IN NMR-SPECTROSCOPY
BENDALL, MR
CARTWRIGHT, IL
LOWE, G
NURSE, D
CLARK, PI
[J]. EUROPEAN JOURNAL OF BIOCHEMISTRY, 1977, 79 (01): : 201 - 209
[7] Brocklehurst K., 1987, HYDROLYTIC ENZYMES, P39
[8] CRYSTALLOGRAPHIC R-FACTOR REFINEMENT BY MOLECULAR-DYNAMICS
BRUNGER, AT
KURIYAN, J
KARPLUS, M
[J]. SCIENCE, 1987, 235 (4787) : 458 - 460
[9] INHIBITION OF CHICKEN CALPAIN-II BY PROTEINS OF THE CYSTATIN SUPERFAMILY AND ALPHA-2-MACROGLOBULIN
CRAWFORD, C
[J]. BIOCHEMICAL JOURNAL, 1987, 248 (02) : 589 - 594
[10] BINDING OF CHLOROMETHYL KETONE SUBSTRATE ANALOGS TO CRYSTALLINE PAPAIN
DRENTH, J
KALK, KH
SWEN, HM
[J]. BIOCHEMISTRY, 1976, 15 (17) : 3731 - 3738

← 1 2 3 →