Gene expression, mutation, and structure-function relationship of scorpion toxin BmP05 active on SKCa channels | |
Wu, JJ ; He, LL ; Zhou, Z ; Chi, CW | |
刊名 | BIOCHEMISTRY |
2002 | |
卷号 | 41期号:8页码:2844-2849 |
关键词 | CA2+-ACTIVATED K+ CHANNELS ADRENAL CHROMAFFIN CELLS NUCLEAR-MAGNETIC-RESONANCE LEIUROTOXIN-I SCYLLATOXIN BUTHUS-MARTENSI KARSCH POTASSIUM CHANNELS GENOMIC ORGANIZATION VENOM PURIFICATION BLOCKER |
ISSN号 | 0006-2960 |
通讯作者 | Chi, CW (reprint author), Chinese Acad Sci, Shanghai Inst Biochem & Cell Biol, State Key Lab Mol Biol, Shanghai 200031, Peoples R China, |
英文摘要 | Four peptide inhibitors of small-conductance Ca2+-activated, apamin-sensitive K+ channels (SKCa) have been isolated from the venom of the Chinese scorpion Buthus martensi, named BmP01, BmP02, BmP03, and BmP05, respectively [Romi-Lebrun, R. (1997) Eur. J. Biochem. 245, 457-464]. Among them BmP05 with 31 amino acid residues has been intensively studied due to its most potent toxicity. To investigate the structure-function relationship of BmP05, its wild type and seven mutants (their C-termini unamidated) were successfully expressed in the yeast secretion system and purified with a high yield over 8 mg/L. Their toxicity to mice and electrophysiological activity on the K+ currents (SKCa and Kv) in rat adrenal chromaffin cells were measured and compared. The results indicated the following: (1) As a selective antagonist against SKCa, 1 muM rBmP05 is equivalent to 0.2 muM apamin, and its IC50 is 0.92 muM. (2) The basic residues Lys and Arg located at positions 6 and 13 in the N-terminal alpha-helix region are essential and synergetic in the interaction of the toxin with SKCa. (3) Disruption of the alpha-helix by mutation of Gln at position 9 with Pro results in almost total loss of toxicity. (4) The C-terminal residue His31 plays an auxiliary role in the interaction of the toxin with SKCa. (5) The beta-turn connecting two beta-sheets near the C-terminal part is responsible for the specificity of the toxin to the different subtypes of K+ channels. |
学科主题 | Biochemistry & Molecular Biology |
收录类别 | SCI |
语种 | 英语 |
公开日期 | 2012-07-23 |
内容类型 | 期刊论文 |
源URL | [http://ir.sibs.ac.cn/handle/331001/2065] |
专题 | 上海神经科学研究所_神经所(总) |
推荐引用方式 GB/T 7714 | Wu, JJ,He, LL,Zhou, Z,et al. Gene expression, mutation, and structure-function relationship of scorpion toxin BmP05 active on SKCa channels[J]. BIOCHEMISTRY,2002,41(8):2844-2849. |
APA | Wu, JJ,He, LL,Zhou, Z,&Chi, CW.(2002).Gene expression, mutation, and structure-function relationship of scorpion toxin BmP05 active on SKCa channels.BIOCHEMISTRY,41(8),2844-2849. |
MLA | Wu, JJ,et al."Gene expression, mutation, and structure-function relationship of scorpion toxin BmP05 active on SKCa channels".BIOCHEMISTRY 41.8(2002):2844-2849. |
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