Cyclic peptide-based potent human SIRT6 inhibitors?
Organic & Biomolecular Chemistry Pub Date: 2016-05-25 DOI: 10.1039/C5OB02339D
Abstract
We discovered in the current study that six side chain-to-side chain cyclic pentapeptides harboring a central Nε-dodecyl (or tetradecyl)-thiocarbamoyl-lysine residue all behaved as highly potent (nM level) inhibitors against human SIRT6-catalyzed deacylation reaction. Moreover, one compound was also found to be selective for SIRT6 versus SIRT2/3/5 (～20-, ～11-, and >940-fold, respectively), despite its modest (～2.3-fold) SIRT6 inhibitory selectivity versus SIRT1. These compounds could be valuable leads for the identification of further potent and selective human SIRT6 inhibitors.
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Journal Name：Organic & Biomolecular Chemistry
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CAS no.: 89640-58-4
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