A FRET-based assay for screening SIRT5 specific modulators

作者：Li Yan; Huang Wenfei; You Ling; Xie Ting; He Bin^*

来源：Bioorganic & Medicinal Chemistry Letters, 2015, 25(8): 1671-1674.

DOI：10.1016/j.bmcl.2015.03.018

• Sirtuin
• Deacetylation
• Desuccinylation
• Fluorogenic assay
• FRET assay

A fluorogenic assay for SIRT5 has been developed to screen their small molecule modulators based on the recent discovery that SIRT5 is a demalonylase and desuccinylase. However, this assay uses a fluorogenic peptide containing 7-amino-4-methylcoumarin (AMC), which becomes the cause of false positive hits from the screening. To overcome this, we have developed an alternative method called a FRET-based assay, which will be reliable and useful for screening SIRT5 modulators in a high-throughput format since no AMC group present in this assay.

• 出版日期2015-4-15
• 单位贵州医科大学