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

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.

authors

Eldefrawi AT,Eldefrawi ME,Konno K,Mansour NA,Nakanishi K,Oltz E,Usherwood PN

doi

10.1073/pnas.85.13.4910

subject

Has Abstract

pub_date

1988-07-01 00:00:00

pages

4910-3

issue

13

eissn

0027-8424

issn

1091-6490

journal_volume

85

pub_type

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