Design, synthesis of allosteric peptide activator for human SIRT1 and its biological evaluation in cellular model of Alzheimer's disease

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• 作者：Rahul Kumar<sup>asup> ; Lokesh Nigam<sup>bsup> ; Amrendra Pratap Singh<sup>asup> ; Kusum Singh<sup>asup> ; Naidu Subbarao<sup>bsup> ; Sharmistha Dey<sup>asup><sup> ; sup><sup>sharmistha_d@hotmail.comsup>
• 关键词：Sirtuin ; Activator ; Peptide ; Aβ25&ndash ; 35 ; IMR-32 ; Allosteric
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：909-916
• 全文大小：1634 K
• 卷排序：127

文摘

CWR as a SIRT1 activator tripeptide by molecular docking. CWR enhanced the activity of recombinant SIRT1 protein by lowering the Michaelis constant, Km. CWR increased the activity of serum sirtuin of Alzheimer's patients. CWR also decreased the acetylation of p53 in IMR32 neuroblastoma cells. CWR protected cell death caused by Aβ amyloid fragments in cell line model of AD.