Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 9, Issue 4, Pages 351-353Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.7b00535
Keywords
Target-guided synthesis; in situ click chemistry; enzyme catalysis; drug discovery
Categories
Funding
- foundation Stiftelsen Olle Engkvist Byggmastare (SOEB)
- Swedish Research Council [2014-04495]
- Swedish Cancer Society [CAN 2016/741]
- Swedish Research Council [2014-04495] Funding Source: Swedish Research Council
- Vinnova [2014-04495] Funding Source: Vinnova
Ask authors/readers for more resources
Finding a new drug candidate for a selected target is an expensive and time-consuming process. Target guided-synthesis, or in situ click chemistry, is a concept where the drug target is used to template the formation of its own inhibitors from reactive building blocks. This could simplify the identification of drug candidates. However, with the exception of one example of an RNA-target, target-guided synthesis has always employed purified targets. This limits the number of targets that can be screened by the method. By applying methods from the field of metabolomics, we demonstrate that target-guided synthesis with protein targets also can be performed directly in cell-based systems. These methods offer new possibilities to conduct screening for drug candidates of difficult protein targets in cellular environments.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available