【摘 要】
：
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 lev
【机 构】
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School of Pharmacy,Jiangsu University,Zhenjiang,212013
【出 处】
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中国生物化学与分子生物学会2016年全国学术会议
论文部分内容阅读
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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