title: A FRET-based assay for screening SIRT6 modulators.
abstract: SIRT6, as one of these seven sirtuins, has been shown to have the therapeutic potentials for treating several human diseases. A fluorogenic assay for SIRT6 has been developed to screen their small molecule modulators based on the recent discovery that SIRT6 is a defatty-acylase (removing long chain fatty acyl groups). However, this assay uses a fluorogenic peptide containing 7-amino-4-methylcoumarin (AMC), which becomes the cause of false positive hits from screenings. To overcome this, we have developed an alternative method called a FRET-based assay suitable for screening SIRT6 modulators, which will be reliable and useful in a high-throughput format since no AMC group present in this assay.
authors.affiliation: College of Basic Medical Science, Guiyang Medical University, Guiyang, Guizhou 550004, China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Li
authors.affiliation: College of Pharmacy, Guiyang Medical University, Guiyang, Guizhou 550004, China; Engineering Research Center for the Development and Application of Ethnic Medicine and TCM, Ministry of Education, Guiyang Medical University, Guiyang, Guizhou 550004, China.
authors.forename: Ling
authors.initials: L
authors.lastname: You
authors.affiliation: College of Pharmacy, Guiyang Medical University, Guiyang, Guizhou 550004, China; Engineering Research Center for the Development and Application of Ethnic Medicine and TCM, Ministry of Education, Guiyang Medical University, Guiyang, Guizhou 550004, China.
authors.forename: Wenfei
authors.initials: W
authors.lastname: Huang
authors.affiliation: State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, Chengdu 610041, China.
authors.forename: Jie
authors.initials: J
authors.lastname: Liu
authors.affiliation: College of Pharmacy, Guiyang Medical University, Guiyang, Guizhou 550004, China; Engineering Research Center for the Development and Application of Ethnic Medicine and TCM, Ministry of Education, Guiyang Medical University, Guiyang, Guizhou 550004, China.
authors.forename: Hong
authors.initials: H
authors.lastname: Zhu
authors.affiliation: College of Pharmacy, Guiyang Medical University, Guiyang, Guizhou 550004, China; Engineering Research Center for the Development and Application of Ethnic Medicine and TCM, Ministry of Education, Guiyang Medical University, Guiyang, Guizhou 550004, China. Electronic address: binhe@gmc.edu.cn.
authors.forename: Bin
authors.initials: B
authors.lastname: He
mesh_terms: D003374:Coumarins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D031541:Fluorescence Resonance Energy Transfer; D005456:Fluorescent Dyes / Q000032:analysis / Q000138:chemical synthesis / Q000737:chemistry; D006801:Humans; D015394:Molecular Structure; D037761:Sirtuins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D003374:Coumarins; D004791:Enzyme Inhibitors; D005456:Fluorescent Dyes; C516592:SIRT6 protein, human; D037761:Sirtuins; C028743:7-amino-4-methylcoumarin
keywords: Deacetylation; Defatty-acylation; FRET assay; Fluorogenic assay; Sirtuin