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Ligand Binding and Linkage00:49

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Allosteric proteins have more than one ligand binding site; the binding of a ligand to any of these sites influences the binding of ligands to the other sites. When a protein is allosteric, its binding sites are called coupled or linked.  In the case of enzymes, the site that binds to the substrate is known as the active site and the other site is known as the regulatory site. When a ligand binds to the regulatory site, this leads to conformational changes in the protein that can influence...
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Transcriptional regulators bind to specific cis-regulatory sequences in the DNA to regulate gene transcription. These cis-regulatory sequences are very short, usually less than ten nucleotide pairs in length. The short length means that there is a high probability of the exact same sequence randomly occurring throughout the genome.  Since regulators can also bind to groups of similar sequences, this further increases the chances of random binding. Transcriptional regulators form...
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Drug-receptor bonds are formed through various chemical forces when drugs interact with target cells. Covalent bonds, strong and irreversible, are exemplified by DNA-alkylating anticancer agents that inhibit cell division. However, such irreversible drug binding lacks selectivity and can modify the DNA of the surrounding healthy cells. Covalent binding often contributes to tissue toxicity, as seen with chloroform and paracetamol metabolites binding to the liver, causing hepatotoxicity.
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Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
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约束着[的约束]

Kaori Mikami-Takei1, Ikuo Yasumasu1

  • 1Department of Biology, School of Education, Waseda University, 1-6-1, Nishiwaseda, Shinjuku-ku, Tokyo 169.

Development, growth & differentiation
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概括

海的精子血膜含有与通道阻断剂结合的蛋白质. 这些用 [3H]二烯来鉴定的蛋白质很可能是电压依赖的通道,类似于哺乳动物细胞中发现的通道.

科学领域:

  • 海洋生物学 海洋生物学
  • 生物化学 生物化学
  • 分子生物学分子生物学

背景情况:

  • 精子等离子膜在受精和细胞过程中起着至关重要的作用.
  • 电压依赖的通道对于调节刺激细胞中的流入至关重要.

研究的目的:

  • 为了识别和描述海精子等离子体膜中的潜在通道.
  • 为了研究特定通道对手与精子膜蛋白的结合.

主要方法:

  • 从四种海精子中分离了血膜分离物.
  • 膜蛋白的电泳分析.
  • 使用 [3H]二烯,一个电压依赖通道对手的结合试验.
  • 竞争性结合研究与尼菲迪平和diltiazem.

主要成果:

  • 在四种海刺物种中观察到类似的电泳特征.
  • 几个精子膜蛋白与 [3H] 二结合,尽管度高于肌肉和神经细胞.
  • 尼菲迪平和迪尔提亚泽姆调节了 [3H] 二与特定蛋白质 (210,140,130,110 kDa) 的结合,表明它们与通道的相互作用.
  • 迪尔蒂亚泽姆的效果模仿了哺乳动物刺激膜中观察到的效果.

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结论:

  • 海的精子血膜中含有蛋白质,其功能是电压依赖的通道.
  • 这些已识别的通道与哺乳动物对应物有相似之处.
  • 这些发现提供了关于海精子中调节的分子机制的见解.