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相关概念视频

Ligand Binding Sites02:40

Ligand Binding Sites

Proteins are dynamic macromolecules that carry out a wide variety of essential processes; however, the activities of most proteins depend on their interactions with other molecules or ions, known as ligands.
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as the...
Ligand Binding and Linkage00:49

Ligand Binding and Linkage

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 the...
Ligand Binding and Linkage00:49

Ligand Binding and Linkage

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 the...
Ligand Binding Sites02:40

Ligand Binding Sites

Proteins are dynamic macromolecules that carry out a wide variety of essential processes; however, the activities of most proteins depend on their interactions with other molecules or ions, known as ligands.
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as the...

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利用DCAF16-SPIN4相互作用来识别PROTAC开发的DCAF16连接体.

Isabella A Riha1, Miguel A Campos1,2, Xiaokang Jin1

  • 1Department of Chemistry, Northwestern University Evanston IL 60208 USA zhang@northwestern.edu.

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研究人员开发了一种新的测定方法,以找到用于向蛋白质降解的DCAF16结合剂. 通过PROTAC技术识别了一种通过PROTAC技术降解FKBP12的化合物,从而推动了药物发现.

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科学领域:

  • 生物化学 生物化学
  • 药用化学 医学化学
  • 分子生物学分子生物学

背景情况:

  • 传统药物向蛋白质活性,但有些蛋白质缺乏合适的位点.
  • 有针对性的蛋白质降解 (TPD) 提供了一个通过指导蛋白质降解的替代方案.
  • DCAF16是一种E3结合酶,通过PROTAC和分子合机制具有TPD的潜力.

研究的目的:

  • 开发一种同质的时间分辨光 (HTRF) 试验,用于发现DCAF16结合剂.
  • 识别与DCAF16.16相互作用的新型化合物.
  • 探索DCAF16结合剂在向蛋白质降解策略中的潜力.

主要方法:

  • 开发一种同质的时间解析光 (HTRF) 试验.
  • 针对DCAF16.6的内部电友图书馆的选.
  • 将DCAF16结合物的化学修饰转化为化向的奇美体 (PROTAC).

主要成果:

  • 鉴定两个与DCAF16结合的二聚体化合物.
  • 一种化合物被发现与DCAF16在cysteines C177-179.9中共聚.
  • 共价DCAF16结合剂已成功转化为一种降解FKBP12的PROTAC.

结论:

  • 开发的HTRF试验对发现DCAF16结合物的有效.
  • DCAF16的共价参与是针对蛋白质降解的可行策略.
  • 这项工作扩大了DCAF16在开发用于治疗应用的新型PROTAC中的实用性.