Structure and synthesis of a potent glutamate receptor antagonist in wasp venom.

A. T. Eldefrawi, M. E. Eldefrawi, K. Konno, N. A. Mansour, K. Nakanishi, E. Oltz, P. N. Usherwood

Research output: Contribution to journalArticle

194 Scopus citations

Abstract

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.

Original languageEnglish
Pages (from-to)4910-4913
Number of pages4
JournalProceedings of the National Academy of Sciences of the United States of America
Volume85
Issue number13
DOIs
StatePublished - Jul 1988

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    Eldefrawi, A. T., Eldefrawi, M. E., Konno, K., Mansour, N. A., Nakanishi, K., Oltz, E., & Usherwood, P. N. (1988). Structure and synthesis of a potent glutamate receptor antagonist in wasp venom. Proceedings of the National Academy of Sciences of the United States of America, 85(13), 4910-4913. https://doi.org/10.1073/pnas.85.13.4910