| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1361723 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
In the current study, we have identified Nε-thiocarbamoyl-lysine (TuAcK) as a general sirtuin inhibitory warhead which was shown to be able to confer potent sirtuin inhibition. This inhibition was also shown to be mechanism-based in that the TuAck residue was able to be processed by a sirtuin enzyme with the formation of a stalled S-alkylamidate intermediate.
Graphical abstractNε-Thiocarbamoyl-lysine (TuAcK), an analog of Nε-acetyl-lysine (AcK), was found in the current study to be able to confer potent sirtuin inhibition. This inhibition was also shown to be mechanism-based.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Brett M. Hirsch, Yujun Hao, Xiaopeng Li, Chrys Wesdemiotis, Zhenghe Wang, Weiping Zheng,