Open AccessStructure and synthesis of a potent glutamate receptor antagonist in wasp venom.
Author(s) -
Amira T. Eldefrawi,
Mohyee E. Eldefrawi,
Katsuhiro Konno,
Nabil Mansour,
Koji Nakanishi,
Eugene M. Oltz,
P.N.R. Usherwood
Publication year - 1988
Publication title -
proceedings of the national academy of sciences of the united states of america
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.011
H-Index - 771
eISSN - 1091-6490
pISSN - 0027-8424
DOI - 10.1073/pnas.85.13.4910
Subject(s) - locust , venom , glutamate receptor , toxin , biology , spermine , antagonist , moiety , nmda receptor , pharmacology , biochemistry , receptor , chemistry , stereochemistry , botany , enzyme
A low molecular weight toxin isolated from the venom of the digger wasp Philanthus triangulum, first noted by T. Piek, is a potent antagonist of transmission at quisqualate-sensitive glutamate synapses of locust leg muscle. This philanthotoxin 433 (PTX-433) has been purified, chemically characterized, and subsequently synthesized along with two closely related analogues. It has a butyryl/tyrosyl/spermine sequence and a molecular weight of 435. Its two analogues, PTX-343 and PTX-334 (the numerals denoting the number of methylenes between the amino groups of the spermine moiety), are also active on the glutamate synapse of the locust leg muscle; PTX-334 was more potent and PTX-343 was less potent than the natural toxin. Such chemicals are useful for studying, labeling, and purifying glutamate receptors and may become models for an additional class of therapeutic drugs and possibly insecticides.