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相关概念视频

Peptide Identification Using Tandem Mass Spectrometry01:33

Peptide Identification Using Tandem Mass Spectrometry

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Tandem mass spectrometry, also known as MS/MS or MS2, is an analytical technique that employs two mass analyzers. Essentially it is a series of mass spectrometers that helps isolate a particular biomolecule and then helps study its chemical properties.
This technique helps gather information regarding the protein from which the peptide was obtained and to study the peptides’ amino acid sequence. Identifying peptides from a complex mixture is an important component of the growing field of...
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MALDI-TOF Mass Spectrometry01:19

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Mass spectrometry is a powerful characterization technique that can identify and separate a wide variety of compounds ranging from chemical to biological entities, based on their mass-to-charge ratio (m/z). The instruments that allow this detection, known as mass spectrometers, have three components: an ion source, a mass analyzer, and a detector. These spectrometers differ based on the nature of their ion source and analyzers.
Matrix-assisted laser desorption ionization (MALDI) is a commonly...
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酶选择性蛋白亲和选择量谱法 (EAS-MS) 的应用.

Xiaoyun Wang1, Jianxian Sun1,2, Shabbir Ahmad2

  • 1Department of Chemistry, University of Toronto, Toronto, ON, Canada.

bioRxiv : the preprint server for biology
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概括

我们开发了对抗选择性蛋白质亲和性选择质谱查 (EAS-MS),以寻找具有挑战性的蛋白质标的弱结合物. 这种方法确定了16个与12个人类蛋白质结合的16个结合物,其中7个显示出对抗选择性结合.

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科学领域:

  • 生物化学 生物化学
  • 化学生物学 化学生物学
  • 药物发现 药物发现 药物发现

背景情况:

  • 对于具有挑战性的蛋白质标来说,识别选择性配体仍然是药物发现中的一个重大障碍.
  • 弱结合剂和酶选择性是传统查方法中经常被忽视的关键因素.

研究的目的:

  • 开发和验证一种酶选择蛋白亲和性选择质谱检测 (EAS-MS) 选方法.
  • 检测弱结合物,并评估对不同的人类蛋白质的连接体选择性.
  • 通过直角测定和结构表征来确认绑定事件.

主要方法:

  • 使用控制蛋白的方法开发.
  • 使用EAS-MS.对8,210种奇拉化合物的查与31种人类蛋白质进行了查.
  • 坐标测定和X射线晶体学用于验证和机械学研究.

主要成果:

  • 发现了16种结合剂,向12种人类蛋白质,包括"挑战性-至-连接物"的标.
  • 鉴定了7种具有3-20μM之间的解离常数 (KDs) 的酶选择性结合剂.
  • 四个标结合体复合物的结构阐明,解释了酶选择性结合的机制.

结论:

  • EAS-MS是一种敏感且高通量的方法,用于识别弱和抗选择性结合剂.
  • 这种方法使得新型和具有挑战性的蛋白质标的配体的表征成为可能.
  • EAS-MS为推进药物发现和化学生物学研究提供了一个强大的工具.