| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1368739 | Bioorganic & Medicinal Chemistry Letters | 2016 | 6 Pages |
Abstract
Transforming a linear pentapeptidic pan-SIRT1/2/3 inhibitor harboring the catalytic mechanism-based sirtuin inhibitory warhead Nε-thioacetyl-lysine into its side chain-to-side chain cyclized derivatives was able to furnish highly potent SIRT1/2/3 inhibition (low nM). This finding attests to the feasibility of developing structurally simple yet highly potent catalytic mechanism-based cyclic peptidic sirtuin inhibitors.
Graphical abstractHighly potent SIRT1/2/3 inhibition was realized by transforming a linear peptidic pan-SIRT1/2/3 inhibitor harboring the catalytic mechanism-based sirtuin inhibitory warhead Nε-thioacetyl-lysine into its cyclized derivatives.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
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Authors
Yajun Huang, Jiajia Liu, Lingling Yan, Weiping Zheng,