title: Specific Turn-On Fluorescent Probe with Aggregation-Induced Emission Characteristics for SIRT1 Modulator Screening and Living-Cell Imaging.
abstract: SIRT1 is an important protein that catalyzes the nicotinamide adenine dinucleotide (NAD)(+)-dependent deacetylation reaction, which is regarded as a novel target to treat metabolic disorders and aging-related diseases. However, there is lack of appropriate approach for SIRT1 modulator screening and bioimaging of SIRT1 in living cells. We designed and synthesized a "turn-on" fluorescent probe by connecting a specifically recognized peptide to tetraphenylethene core. It exhibits excellent selectivity and sensitivity in homogeneous measurement of SIRT1 activity for screening both SIRT1 inhibitors and activators. 20(S)-ginsenoside Rg3 and ophiopogonin D' were found to activate SIRT1. It was also successfully applied to monitor SIRT1 modulation in the cardiomyocytes as well as in the wild-type and SIRT1(-/-) mesenchymal stem cells.
authors.affiliation: †College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang China.
authors.forename: Yi
authors.initials: Y
authors.lastname: Wang
authors.affiliation: †College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang China.
authors.forename: Yaqi
authors.initials: Y
authors.lastname: Chen
authors.affiliation: †College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang China.
authors.forename: Haibo
authors.initials: H
authors.lastname: Wang
authors.affiliation: †College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang China.
authors.forename: Yiyu
authors.initials: Y
authors.lastname: Cheng
authors.affiliation: ‡College of Preclinical Medicine, Zhejiang Chinese Medical University, Hangzhou, Zhejiang China.
authors.forename: Xiaoping
authors.initials: X
authors.lastname: Zhao
mesh_terms: D000107:Acetylation; D000818:Animals; D002460:Cell Line; D002470:Cell Survival; D004789:Enzyme Activation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000494:pharmacology; D005456:Fluorescent Dyes / Q000737:chemistry*; D006801:Humans; D057054:Molecular Imaging / Q000379:methods*; D032383:Myocytes, Cardiac / Q000166:cytology; D051381:Rats; D056564:Sirtuin 1 / Q000037:antagonists & inhibitors* / Q000378:metabolism*
chemical_list: D004791:Enzyme Inhibitors; D005456:Fluorescent Dyes; C488368:Sirt1 protein, rat; D056564:Sirtuin 1