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对表观遗传相关支架的以为导向的合成

Timothé Maujean¹, Prakash Kannaboina¹, Adam I Green¹

¹Department of Biochemistry and Biophysics, Department of Cancer Biology and Epigenetics Institute, Perelman School of Medicine, University of Pennsylvania, PA 19104, USA. George.Burslem@Pennmedicine.upenn.edu.

Chemical communications (Cambridge, England)

|November 22, 2023

概括

一种新的方法使用连续函数对分子的状性进行排名,其性能优于现有的方法. 这有助于发现用于表观遗传标的候选药物,如HDAC6,BRD4和EZH2.2.

科学领域:

药用化学医学化学
药物发现药物发现药物发现
表观遗传学在表观遗传学中,表观遗传学是指表观遗传学.

背景情况:

的类似性对于药物发现至关重要,指导着有前途的分子的选择.
现有的评估与相似性的方法可能很复杂或缺乏持续评估.
诸如HDAC6,BRD4和EZH2之类的表观遗传点是治疗干预的关键领域.

研究的目的:

开发一种简单,合理的方法来排列分子的性.
应用持续评估功能,以更细致地评估分子性质.
引导合成工作向针对表观遗传标的新药候选人.

主要方法:

基于持续评估功能的新排名策略的开发.
对新方法的比较分析与已建立的类似性评估技术进行比较.
应用该方法来识别针对特定表观遗传点的潜在候选药物.

主要成果:

开发的方法提供了一种简单而合理的方法来排列分子相似性.
与现有方法相比,该战略显示出具有竞争力的表现.
这种方法成功地将合成努力引导到有希望的表观遗传药物候选者.

结论:

新的持续评估函数方法对于排名领先相似性是有效的.
这种策略在药物发现工作流程中提供了竞争优势.
该方法有助于识别针对HDAC6,BRD4和EZH2的分子,用于表观遗传应用.

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