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相关概念视频

Targeted Cancer Therapies02:57

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The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
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Author Spotlight: Network Pharmacology and Molecular Docking to Decipher the Action of Jiawei Shengjiang San Against Diabetic Kidney Disease
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针对癌症点Jumonji-C域含有蛋白6的分析抑制剂架构.

Thomas P Corner1, Eidarus Salah1, Anthony Tumber1

  • 1Chemistry Research Laboratory, Department of Chemistry and the Ineos Oxford Institute for Antimicrobial Research, University of Oxford, 12 Mansfield Road, Oxford, OX1 3TA, UK.

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概括

研究人员开发了一种新的测定方法,以寻找JMJD6抑制剂用于前列腺癌治疗. 一些用于其他疾病的现有药物有效抑制JMJD6,这表明了新的治疗途径.

关键词:
2 - 氧格酸盐/α - 基酸盐依赖的氧化酶.他们决定重建国家.美国国家统计局JmjC 抑制基酶的作用朱蒙吉-C域-含有蛋白6的蛋白质含 bromodomain 的蛋白质 4 的蛋白质.高通量抑制试验的高通量抑制试验抑制剂的发现发现.转移性割抵抗性前列腺癌

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科学领域:

  • 生物化学 生化学
  • 分子生物学分子生物学
  • 在瘤学瘤学.

背景情况:

  • 含有 Jumonji-C 域的蛋白6 (JMJD6) 是一种参与翻译后修改的人类酶.
  • 失调的JMJD6活性与雄激素受体结合变异7 (AR-V7) 的上调相关,这是一个驱动前列腺癌抗雄激素疗法耐药性的机制.
  • 由于JMJD6在治疗耐药性方面的作用,被认为是前列腺癌的潜在治疗标.

研究的目的:

  • 建立和验证一种可靠的测定方法,用于选小分子抑制剂的孤立JMJD6.6.
  • 识别具有开发选择性JMJD6抑制剂潜力的新型化学支架.
  • 调查已知JMJD6抑制剂和临床药物的抑制活性,针对孤立的JMJD6.

主要方法:

  • 开发结合质谱法 (SPE-MS) 试验的固相提取方法,用于监测JMJD6的催化活性.
  • 使用开发的SPE-MS测定方法对之前报告的JMJD6抑制剂 (WL12,SKLB325,化合物7p) 的查.
  • 对临床使用的含蛋白 (PHD) 抑制剂 (Enarodustat,Desidustat) 对单独的JMJD6.6进行体外抑制作用的评估.

主要成果:

  • 开发的SPE-MS试验提供了一种可靠的方法来评估小分子抑制JMJD6.
  • 以前报告的JMJD6抑制剂在体外显示出有限的疗效.
  • 一些临床PHD抑制剂,特别是Enarodustat和Desidustat,表现出强烈的抑制孤立的JMJD6.
  • 这表明JMJD6抑制可能是这些临床使用的PHD抑制剂的非目标效应.

结论:

  • 这项研究提供了一种有效的测定方法,用于识别和表征JMJD6抑制剂.
  • 确定了开发选择性和细胞透性JMJD6抑制剂的有吸引力的化学支架.
  • 这些发现表明,JMJD6抑制可能是临床环境中使用某些PHD抑制剂的意外后果,需要进一步调查.