Expanding the scope of metal catalysed DNA-encoded library synthesis

扩大金属催化 DNA 编码文库合成的范围

• 批准号: 2281957
• 金额: --
• 依托单位: Newcastle University
• 依托单位国家: 英国
• 项目类别: Studentship
• 财政年份: 2019
• 资助国家: 英国
• 起止时间: 2019 至 无数据
• 项目状态: 已结题
• 来源: https://gtr.ukri.org/projects?ref=studentship-2281957
• 关键词: Expanding; scope; metal; catalysed; DNA

DNA encoded libraries (DELs) offer an exciting new technology for the rapid and cost-effective identification of hit compounds for drug discovery and chemical biology. Currently the libraries of compounds available to screen are limited by the range of chemistry that can be carried out on DNA-conjugated substrates. We will expand the chemistry available for generating DELs using new approaches to a range of metal-catalysed transformations, including reactions that are unreliable under traditional DEL conditions. The methodology will be applied to DEL synthesis to establish the scope and to generate libraries for screening against novel protein targets.

DNA编码文库（DELs）为药物发现和化学生物学提供了一种令人兴奋的快速和经济有效的鉴定命中化合物的新技术。目前，可用于筛选的化合物库受到可以在DNA缀合的底物上进行的化学范围的限制。我们将使用新方法扩展可用于生成DEL的化学方法，以实现一系列金属催化转化，包括在传统DEL条件下不可靠的反应。该方法将应用于DEL合成，以建立范围并生成用于筛选新蛋白质靶点的文库。

项目成果

Highly efficient on-DNA amide couplings promoted by micelle forming surfactants for the synthesis of DNA encoded libraries.

• DOI: 10.1039/d1sc03007h
• 发表时间: 2021-07-14
• 期刊: Chemical science
• 影响因子: 8.4
• 作者: Hunter JH;Anderson MJ;Castan IFSF;Graham JS;Salvini CLA;Stanway-Gordon HA;Crawford JJ;Madin A;Pairaudeau G;Waring MJ
• 通讯作者: Waring MJ

On-DNA Transfer Hydrogenolysis and Hydrogenation for the Synthesis of DNA-Encoded Chemical Libraries.

DNA转移氢解和氢化，用于合成DNA编码的化学文库。

• DOI: 10.1002/anie.202111927
• 发表时间: 2022-01-17
• 期刊: ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
• 影响因子: 16.6
• 作者: Stanway-Gordon, Harriet A.;Graham, Jessica S.;Waring, Michael J.
• 通讯作者: Waring, Michael J.

On-DNA Transfer Hydrogenolysis and Hydrogenation for the Synthesis of DNA-Encoded Chemical Libraries

DNA 转移氢解和氢化用于合成 DNA 编码的化学文库

• DOI: 10.1002/ange.202111927
• 发表时间: 2021
• 期刊: Angewandte Chemie
• 作者: Stanway-Gordon H