In this section, you can access to the latest technical information related to the FUTURE project topic.

The mimics of N?-acyl-lysine derived from cysteine as sirtuin inhibitors

Sirtuin inhibitors as physiological research tools and therapeutic potentials have caught many attentions in last decades. The mimics of acyl lysine have been approved to be a very efficient strategy for development of mechanism-based sirtuin inhibitors. In current study, a novel scaffold of l-S-(3-carboxamidopropyl) cysteine (l-CAPC) has been exploited for design and synthesis of sirtuin inhibitors. As a result, the mimics of N?-acyl-lysine derived from cysteine including small molecules (5a–m) and peptides (9a–m) have been synthesized. Among these, the peptides 9g and 9h were found to be the most inhibitory potency and selectivity against SIRT2.

» Author: Chun Wang, Fang Wang, Xiaoxue Chen, Yefang Zou, Hong Zhu, Qingjie Zhao, Jingshan Shen, Yan Li, Yongjun Li, Bin He

» Reference: 10.1016/j.bmcl.2018.06.030

» Publication Date: 01/08/2018

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