Synthesis and paralytic activities of squaryl amino acid-containing polyamine toxins.
T Shinada, Y Nakagawa, K Hayashi, G Corzo, T Nakajima, Y Ohfune
Index: Amino Acids 24(3) , 293-301, (2003)
Full Text: HTML
Abstract
Eight analogs 4A-7A and 4B-7B of philanthotoxin (PhTX) from wasp venom and nephilatoxin-8 (NPTX-8) from spider venom whose tyrosine or asparagine linker is replaced by squaryl (sq) amino acid or 4-amino squaryl (4-asq) amino acid have been synthesized in an efficient manner via coupling of N-acyl squaryl amino acid intermediate 19 or 26 with the corresponding polyamine part. Preliminary bioassay using crickets revealed that the analogs substituted by glutamate-type squaryl amino acid-containing NPTX 7A and 7B showed more potent paralytic activities than that of NPTX-8.
Related Compounds
Related Articles:
Open-channel blockade is less effective on GluN3B than GluN3A subunit-containing NMDA receptors
2012-07-05
[Eur. J. Pharmacol. 686(1-3) , 22-31, (2012)]
1996-01-19
[J. Med. Chem. 39(2) , 515-21, (1996)]
A sequential high-yielding large-scale solution-method for synthesis of philanthotoxin analogues.
2003-01-01
[Eur. J. Med. Chem. 38(1) , 117-22, (2003)]
1997-09-01
[Br. J. Pharmacol. 122(2) , 379-85, (1997)]
2000-01-01
[Receptors Channels 7(3) , 227-36, (2000)]