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Molecules 2016, 21(9), 1217;

A Selective Cyclic Peptidic Human SIRT5 Inhibitor

School of Pharmacy, Jiangsu University, 301 Xuefu Road, Zhenjiang 212013, Jiangsu Province, China
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 25 July 2016 / Revised: 5 September 2016 / Accepted: 5 September 2016 / Published: 10 September 2016
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In the current study, we discovered that a side chain-to-side chain cyclic pentapeptide harboring a central Nε-carboxyethyl-thiocarbamoyl-lysine residue behaved as a strong and selective (versus human SIRT1/2/3/6) inhibitor against human SIRT5-catalyzed deacylation reaction. This compound was also found to be proteolytically much more stable than its linear counterpart. This compound could be a valuable lead for developing stronger, selective, metabolically stable, and cell permeable human SIRT5 inhibitors. View Full-Text
Keywords: sirtuin; SIRT5; inhibitor; cyclic peptide; Nε-carboxyethyl-thiocarbamoyl-lysine sirtuin; SIRT5; inhibitor; cyclic peptide; Nε-carboxyethyl-thiocarbamoyl-lysine

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Liu, J.; Huang, Y.; Zheng, W. A Selective Cyclic Peptidic Human SIRT5 Inhibitor. Molecules 2016, 21, 1217.

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