SYNTHESIS OF OMEGA-AGATOXIN IVA AND ITS RELATED PEPTIDES

被引：25

作者：

NISHIO, H

KUMAGAYE, KY

KUBO, S

CHEN, YN

MOMIYAMA, A

TAKAHASHI, T

KIMURA, T

SAKAKIBARA, S

机构：

[1] PROT RES FDN,PEPTIDE INST INC,MINO,OSAKA 562,JAPAN

[2] UNIV TOKYO,INST BRAIN RES,DEPT NEUROPHYSIOL,TOKYO 113,JAPAN

[3] KYOTO UNIV,FAC MED,DEPT PHYSIOL,KYOTO 606,JAPAN

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1993年 / 196卷 / 03期

关键词：

D O I：

10.1006/bbrc.1993.2414

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A potent and selective P type calcium channel blocker isolated from the venom of the funnel web spider Agelenopsis aperta, ω-agatoxin IVA, and its related peptides were synthesized by the solution procedure. Synthetic ω-agatoxin IVA was found to block high-threshold P-type calcium current in rat Purkinje neuron with the same potency as that reported for the natural products. Its disulfide structure was determined by amino acid analysis, gas-phase sequencing and mass spectrometry of the proteolytic fragments. The N-terminus biotinylated and truncated peptides showed the same disulfide-bond-forming profile and the same activities as those of ω-agatoxin IVA, indicating that the N-terminal basic tripeptide, Lys-Lys-Lys, is not important for both the folding and the expression of the biological activity. However, the Trp residue in the molecule might be essential for the toxin to bind tightly with the channel pores. © 1993 Academic Press, Inc.

引用

页码：1447 / 1453

页数：7

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