BmK-YA, an enkephalin-like peptide in scorpion venom.

BmK-YA, an enkephalin-like peptide in scorpion venom.
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DOI:
10.1371/journal.pone.0040417
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发表时间:
2012
期刊:
影响因子:
3.7
通讯作者:
Civelli O
Civelli O
中科院分区:
综合性期刊3区
文献类型:
--
作者:
Zhang Y;Xu J;Wang Z;Zhang X;Liang X;Civelli O

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通过筛选亚洲蝎子Buthus martensii Karsch (BmK)毒液提取物激活阿片受体的能力,我们鉴定了BmK- ya,一种含有脑啡肽样序列的修饰肽。BmK-YA由一个前体编码,该前体显示一个信号序列,包含BmK-YA序列的四个拷贝和His4-BmK-YA的四个拷贝,它们的两侧都有单个氨基酸残基。BmK-YA和His4-BmK-YA经过修饰,符合生物活性肽的特性。BmK-YA可选择性激活哺乳动物阿片受体δ亚型,而His4-BmK-YA对阿片受体无活性。BmK-YA的发现表明,蝎子毒液可能是一种靶向G蛋白偶联受体(gpcr)的生物活性分子的新来源,并为阿片前体的进化提供了新的见解。
By screening extracts of venom from the Asian scorpion Buthus martensii Karsch (BmK) for their abilities to activate opioid receptors, we have identified BmK-YA, an amidated peptide containing an enkephalin-like sequence. BmK-YA is encoded by a precursor that displays a signal sequence and contains four copies of BmK-YA sequences and four of His4-BmK-YA, all flanked by single amino acid residues. BmK-YA and His4-BmK-YA are amidated and thus fulfill the characteristics expected of bioactive peptides. BmK-YA can activate mammalian opioid receptors with selectivity for the δ subtype while His4-BmK-YA is inactive at opioid receptors. The discovery of BmK-YA suggests that scorpion venom may represent a novel source of bioactive molecules targeting G protein-coupled receptors (GPCRs) and reveal additional insights on the evolution of the opioid precursors.
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