High-resolution X-ray crystallography reveals precise binding interactions between human nonpancreatic secreted phospholipase A(2) and a highly potent inhibitor (FPL67047XX)

被引:36
作者
Cha, SS
Lee, D
Adams, J
Kurdyla, JT
Jones, CS
Marshall, LA
Bolognese, B
AbdelMeguid, SS
Oh, BH
机构
[1] SMITHKLINE BEECHAM PHARMACEUT, DEPT MACROMOL SCI, KING OF PRUSSIA, PA 19406 USA
[2] SMITHKLINE BEECHAM PHARMACEUT, DEPT MED CHEM, KING OF PRUSSIA, PA 19406 USA
[3] SMITHKLINE BEECHAM PHARMACEUT, DEPT BIOCHEM, KING OF PRUSSIA, PA 19406 USA
[4] SMITHKLINE BEECHAM PHARMACEUT, DEPT INFLAMMAT & RESP PHARMACOL, KING OF PRUSSIA, PA 19406 USA
[5] POHANG UNIV SCI & TECHNOL, DEPT LIFE SCI, KYUNGBUK 790784, SOUTH KOREA
关键词
D O I
10.1021/jm960502g
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
[No abstract available]
引用
收藏
页码:3878 / 3881
页数:4
相关论文
共 30 条
[21]   ARE EVENTS AFTER ENDOTOXEMIA RELATED TO CIRCULATING PHOSPHOLIPASE A(2) [J].
SANTOS, AA ;
BROWNING, JL ;
SCHELTINGA, MR ;
LYNCH, EA ;
BROWN, EF ;
LAWTON, P ;
CHAMBERS, E ;
DOUGAS, I ;
BENJAMIN, CD ;
DINARELLO, CA ;
WOLFF, SM ;
JACOBS, DO ;
WILMORE, DW .
ANNALS OF SURGERY, 1994, 219 (02) :183-192
[22]   STRUCTURE-BASED DESIGN OF THE FIRST POTENT AND SELECTIVE INHIBITOR OF HUMAN NONPANCREATIC SECRETORY PHOSPHOLIPASE-A(2) [J].
SCHEVITZ, RW ;
BACH, NJ ;
CARLSON, DG ;
CHIRGADZE, NY ;
CLAWSON, DK ;
DILLARD, RD ;
DRAHEIM, SE ;
HARTLEY, LW ;
JONES, ND ;
MIHELICH, ED ;
OLKOWSKI, JL ;
SNYDER, DW ;
SOMMERS, C ;
WERY, JP .
NATURE STRUCTURAL BIOLOGY, 1995, 2 (06) :458-465
[23]   STRUCTURES OF FREE AND INHIBITED HUMAN SECRETORY PHOSPHOLIPASE-A2 FROM INFLAMMATORY EXUDATE [J].
SCOTT, DL ;
WHITE, SP ;
BROWNING, JL ;
ROSA, JJ ;
GELB, MH ;
SIGLER, PB .
SCIENCE, 1991, 254 (5034) :1007-1010
[24]   CRYSTAL-STRUCTURE OF BEE-VENOM PHOSPHOLIPASE-A2 IN A COMPLEX WITH A TRANSITION-STATE ANALOG [J].
SCOTT, DL ;
OTWINOWSKI, Z ;
GELB, MH ;
SIGLER, PB .
SCIENCE, 1990, 250 (4987) :1563-1566
[25]  
SEILHAMER JJ, 1989, J BIOL CHEM, V264, P5335
[26]   X-RAY STRUCTURE OF PHOSPHOLIPASE-A2 COMPLEXED WITH A SUBSTRATE-DERIVED INHIBITOR [J].
THUNNISSEN, MMGM ;
AB, E ;
KALK, KH ;
DRENTH, J ;
DIJKSTRA, BW ;
KUIPERS, OP ;
DIJKMAN, R ;
DEHAAS, GH ;
VERHEIJ, HM .
NATURE, 1990, 347 (6294) :689-691
[27]  
VANDENBERG B, 1995, BIOMOL NMR, V5, P10
[28]   COMPETITIVE-INHIBITION OF LIPOLYTIC ENZYMES .6. INHIBITION OF 2 HUMAN PHOSPHOLIPASES-A2 BY ACYLAMINO PHOSPHOLIPID ANALOGS [J].
VANDENBERG, L ;
FRANKEN, PA ;
VERHEIJ, HM ;
DIJKMAN, R ;
DEHAAS, GH .
BIOCHIMICA ET BIOPHYSICA ACTA, 1992, 1124 (01) :66-70
[29]   CRYSTAL-STRUCTURE OF COBRA-VENOM PHOSPHOLIPASE-A2 IN A COMPLEX WITH A TRANSITION-STATE ANALOG [J].
WHITE, SP ;
SCOTT, DL ;
OTWINOWSKI, Z ;
GELB, MH ;
SIGLER, PB .
SCIENCE, 1990, 250 (4987) :1560-1563
[30]   CRITICAL ROLE OF A HYDROGEN-BOND IN THE INTERACTION OF PHOSPHOLIPASE-A2 WITH TRANSITION-STATE AND SUBSTRATE-ANALOGS [J].
YU, L ;
DENNIS, EA .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1991, 88 (20) :9325-9329