PHILANTHOTOXIN-433 (PHTX-433), A NONCOMPETITIVE GLUTAMATE RECEPTOR INHIBITOR

被引：47
作者：
NAKANISHI, K
GOODNOW, R
KONNO, K
NIWA, M
BUKOWNIK, R
KALLIMOPOULOS, TA
USHERWOOD, P
ELDEFRAWI, AT
ELDEFRAWI, ME
机构：
[1] UNIV NOTTINGHAM,DEPT ZOOL,NOTTINGHAM NG7 2RD,ENGLAND
[2] UNIV MARYLAND,SCH MED,BALTIMORE,MD 21201
来源：
PURE AND APPLIED CHEMISTRY | 1990年 / 62卷 / 07期
关键词：
D O I：
10.1351/pac199062071223
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
A polyamine toxin present in the venom sac of the solitary digger wasp Philanthus triangulum, first noted by T. Piek, has been isolated, characterized, and synthesized. This toxin, philanthotoxin-433 (PhTX-433), having a butyryl/tyrosyl/polyamine structure, is a potent noncompetitive inhibitor of the quisqualate sub-type glutamate receptor as assayed by the twitch contraction of locust leg muscles. It is also an allosteric inhibitor of acetylcholine receptors of vertebrates. About sixty analogs of PhTX have been synthesized in order to clarify structure/activity relationships and to select candidates suitable for isolating the glutamate receptor by photoaffinity label and/or affinity label. © 1990 IUPAC
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页码：1223 / 1230
页数：8
相关论文
共 21 条
[1]   STRUCTURES AND BIOLOGICAL-ACTIVITIES OF 3 SYNAPTIC ANTAGONISTS FROM ORB WEAVER SPIDER VENOM [J].
ADAMS, ME ;
CARNEY, RL ;
ENDERLIN, FE ;
FU, ET ;
JAREMA, MA ;
LI, JP ;
MILLER, CA ;
SCHOOLEY, DA ;
SHAPIRO, MJ ;
VENEMA, VJ .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1987, 148 (02) :678-683
[2]   CHEMICAL CHARACTERIZATION OF SPIDER TOXIN, JS']JSTX AND NSTX [J].
ARAMAKI, Y ;
YASUHARA, T ;
HIGASHIJIMA, T ;
YOSHIOKA, M ;
MIWA, A ;
KAWAI, N ;
NAKAJIMA, T .
PROCEEDINGS OF THE JAPAN ACADEMY SERIES B-PHYSICAL AND BIOLOGICAL SCIENCES, 1986, 62 (09) :359-362
[3]   MOLECULAR-BIOLOGY OF THE GABA-A RECEPTOR - THE RECEPTOR CHANNEL SUPERFAMILY [J].
BARNARD, EA ;
DARLISON, MG ;
SEEBURG, P .
TRENDS IN NEUROSCIENCES, 1987, 10 (12) :502-509
[4]  
BRUCE M, IN PRESS TOXICON
[5]   THE ACETYLCHOLINE-RECEPTOR MOLECULE - ALLOSTERIC SITES AND THE ION CHANNEL [J].
CHANGEUX, JP ;
REVAH, F .
TRENDS IN NEUROSCIENCES, 1987, 10 (06) :245-250
[6]   EXCITATORY AMINO-ACIDS IN THE BRAIN - FOCUS ON NMDA RECEPTORS [J].
COTMAN, CW ;
IVERSEN, LL .
TRENDS IN NEUROSCIENCES, 1987, 10 (07) :263-265
[7]   STRUCTURE AND SYNTHESIS OF A POTENT GLUTAMATE RECEPTOR ANTAGONIST IN WASP VENOM [J].
ELDEFRAWI, AT ;
ELDEFRAWI, ME ;
KONNO, K ;
MANSOUR, NA ;
NAKANISHI, K ;
OLTZ, E ;
USHERWOOD, PNR .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1988, 85 (13) :4910-4913
[8]   ACIDIC AMINO-ACID BINDING-SITES IN MAMMALIAN NEURONAL MEMBRANES - THEIR CHARACTERISTICS AND RELATIONSHIP TO SYNAPTIC RECEPTORS [J].
FOSTER, AC ;
FAGG, GE .
BRAIN RESEARCH REVIEWS, 1984, 7 (02) :103-164
[9]  
GOODNOW R, IN PRESS TETRAHEDRON
[10]  
GRISHIN EV, 1986, BIOORG KHIM+, V12, P1121
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