Designing Chimeric Molecules for Drug Discovery by Leveraging Chemical Biology.,Journal of Medicinal Chemistry

当前位置： X-MOL 学术 › J. Med. Chem. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Designing Chimeric Molecules for Drug Discovery by Leveraging Chemical Biology.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-02-19 , DOI: 10.1021/acs.jmedchem.9b01456
Chiara Borsari ₁ , Darci J Trader ₂ , Annalisa Tait ₃ , Maria P Costi ₃

Affiliation

After the first seed concept introduced in the 18th century, different disciplines have attributed different names to dual-functional molecules depending on their application, including bioconjugates, bifunctional compounds, multitargeting molecules, chimeras, hybrids, engineered compounds. However, these engineered constructs share a general structure: a first component that targets a specific cell and a second component that exerts the pharmacological activity. A stable or cleavable linker connects the two modules of a chimera. Herein, we discuss the recent advances in the rapidly expanding field of chimeric molecules leveraging chemical biology concepts. This Perspective is focused on bifunctional compounds in which one component is a lead compound or a drug. In detail, we discuss chemical features of chimeric molecules and their use for targeted delivery and for target engagement studies.

中文翻译：

通过利用化学生物学设计用于药物发现的嵌合分子。

在18世纪首次提出种子概念之后，不同学科根据双功能分子的应用将不同的名称赋予双功能分子，包括生物缀合物，双功能化合物，多靶分子，嵌合体，杂种，工程化合物。但是，这些工程改造的构建体具有一个总体结构：靶向特定细胞的第一组分和发挥药理活性的第二组分。稳定或可裂解的连接子连接嵌合体的两个模块。在此，我们讨论利用化学生物学概念在嵌合分子迅速扩展领域中的最新进展。本观点着眼于双功能化合物，其中一种成分是先导化合物或药物。详细，

更新日期：2020-02-19

点击分享查看原文

点击收藏

阅读更多本刊最新论文本刊介绍/投稿指南11