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Structural investiga tions for developing therapeutics of functional disorders due to the sodium channel

Structural investiga tions for developing therapeutics of functional disorders due to the sodium channel
开发钠通道功能障碍疗法的结构研究
批准号:
09470493
负责人:
KURODA Yoshihiro
金额:
$8.58万
依托单位:
依托单位国家:
日本
项目类别:
Grant-in-Aid for Scientific Research (B)
财政年份:
1997
资助国家:
日本
项目状态:
已结题
起止时间:
1997 至 1999

项目摘要

项目成果

KURODA Yoshihiro的其他基金

相关文献

中文摘要
翻译
1. 叔胺型局部麻醉药在生理条件下具有电荷,与III-IV连接体的疏水基序IMF中的苯丙氨酸残基疏水相互作用,也与IMF基序前后的酸性氨基酸残基静电相互作用。在与上述相似的条件下,苯佐卡因与叔胺型局部胺一样位于极头基团区域,但不能与III-IV连接体相互作用。IMF基元周围的结构一般为α-螺旋结构。IMF基序周围的结构是由IMF中异亮氨酸和苏氨酸之间的氢键控制的,苏氨酸位于IMF残基之后。五肽KIFMK与III-IV连接体特异性相互作用,稳定了IMF基序结构周围的α-螺旋结构。作为治疗苏氨酸突变为蛋氨酸的先天性副肌张力症(PMC)的药物,认为一种能够稳定野生型钠中IFMT基序形成的α-螺旋结构的分子可能是一种很好的药物。
英文摘要
1. The tertiary amine type local anesthetics which possess a charge under physiological conditions interact hydrophobically with the phenylalanine residue in the hydrophobic motif, IMF, of the III-IV linker and also electrostatically with the acidic amino acid residues which locate before and after the IMF motif.2. At a similar condition as above, benzocaine locates at a polarhead-group region as in the case of the tertiary amine type local anes the tics, but cannot interact with the III-IV linker.3. The structure at around the IMF motifis generally α-helical. The structure at around the IMF motifis controlled by a hydrogen bonding between the isoleucine in the IMF and the threonine which take a position just after the IMF residues.4. A pentapeptide KIFMK interacts specifically with the III-IV linker and stabilizes the α-helical structure at around the structure of the IMF motif.As a therapeutic for paramyotonia congenita (PMC), in which the threonine is mutated into methionine, it is considered that a molecule which can stabilize the α-helical structure formed by the IFMT motifin the wild type sodium can be a good drug.
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Yoshihiro Kuroda: "ィイD11ィエD1H-NMR and circular dichroism spectroscopic studies on changes in secondary structures of the sodium channel in activation gate peptides as ca us ed by the pentapep tide KIFMK"Biophysical Journal. 77. 1363-1373 (1999)
Yoshihiro Kuroda:“由五肽 KIFMK 引起的激活门肽中钠通道二级结构变化的 D11D1H-NMR 和圆二色性光谱研究”生物物理学杂志 77. 1363-1373 (1999)。
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High quality haptic interaction with a soft body for remote collaboration
  • 批准号:
    24700117
  • 项目类别:
    Grant-in-Aid for Young Scientists (B)
  • 资助金额:
    $2.75万
  • 财政年份:
    2012
  • 负责人:
    KURODA Yoshihiro
  • 依托单位:
The inhibitory potency of peptides derived from autophosphorylation sites of receptor tyrosine kinase in a non-ATP-competitive mechanism on tumor cells.
  • 批准号:
    22590076
  • 项目类别:
    Grant-in-Aid for Scientific Research (C)
  • 资助金额:
    $2.91万
  • 财政年份:
    2010
  • 负责人:
    KURODA Yoshihiro
  • 依托单位:
Studies on inhibitors for epidermal growth factor receptor based on oligopeptides which imitated pseudosubstrates
Mechanisms of suppression of insulin signaling by Na channel blockers
  • 批准号:
    15590040
  • 项目类别:
    Grant-in-Aid for Scientific Research (C)
  • 资助金额:
    $1.92万
  • 财政年份:
    2003
  • 负责人:
    KURODA Yoshihiro
  • 依托单位: