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

引用

页码：1223 / 1230

页数：8

共 21 条

[1] STRUCTURES AND BIOLOGICAL-ACTIVITIES OF 3 SYNAPTIC ANTAGONISTS FROM ORB WEAVER SPIDER VENOM
ADAMS, ME
CARNEY, RL
ENDERLIN, FE
FU, ET
JAREMA, MA
LI, JP
MILLER, CA
SCHOOLEY, DA
SHAPIRO, MJ
VENEMA, VJ
[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1987, 148 (02) : 678 - 683
[2] CHEMICAL CHARACTERIZATION OF SPIDER TOXIN, JS']JSTX AND NSTX
ARAMAKI, Y
YASUHARA, T
HIGASHIJIMA, T
YOSHIOKA, M
MIWA, A
KAWAI, N
NAKAJIMA, T
[J]. 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
BARNARD, EA
DARLISON, MG
SEEBURG, P
[J]. 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
CHANGEUX, JP
REVAH, F
[J]. TRENDS IN NEUROSCIENCES, 1987, 10 (06) : 245 - 250
[6] EXCITATORY AMINO-ACIDS IN THE BRAIN - FOCUS ON NMDA RECEPTORS
COTMAN, CW
IVERSEN, LL
[J]. TRENDS IN NEUROSCIENCES, 1987, 10 (07) : 263 - 265
[7] STRUCTURE AND SYNTHESIS OF A POTENT GLUTAMATE RECEPTOR ANTAGONIST IN WASP VENOM
ELDEFRAWI, AT
ELDEFRAWI, ME
KONNO, K
MANSOUR, NA
NAKANISHI, K
OLTZ, E
USHERWOOD, PNR
[J]. 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
FOSTER, AC
FAGG, GE
[J]. 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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