title: Environment-Sensitive Fluorescent Probe for the Human Ether-a-go-go-Related Gene Potassium Channel.
abstract: A novel environment-sensitive probe S2 with turn-on switch for Human Ether-a-go-go-Related Gene (hERG) potassium channel was developed herein. After careful evaluation, this fluorescent probe showed high binding affinity with hERG potassium channel with an IC50 value of 41.65 nM and can be well applied to hERG channel imaging or cellular distribution study for hERG channel blockers. Compared with other imaging techniques, such as immunofluorescence and fluorescent protein-based approaches, this method is convenient and affordable, especially since a washing procedure is not needed. Meanwhile, this environment-sensitive turn-on design strategy may provide a good example for the probe development for these targets that have no reactive or catalytic activity.
authors.affiliation: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University , Jinan, Shandong 250012, China.
authors.forename: Zhenzhen
authors.initials: Z
authors.lastname: Liu
authors.affiliation: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University , Jinan, Shandong 250012, China.
authors.forename: Tianyu
authors.initials: T
authors.lastname: Jiang
authors.affiliation: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University , Jinan, Shandong 250012, China.
authors.forename: Beilei
authors.initials: B
authors.lastname: Wang
authors.affiliation: Laboratory of Anaesthesiology and Critical Care Medicine, West China Hospital, Sichuan University , Chengdu, Sichuan 610041, China.
authors.forename: Bowen
authors.initials: B
authors.lastname: Ke
authors.affiliation: Institute of Biosciences and Technology, Texas A&M University Health Science Center , Houston, Texas 77030, United States.
authors.forename: Yubin
authors.initials: Y
authors.lastname: Zhou
authors.affiliation: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University , Jinan, Shandong 250012, China.
authors.forename: Lupei
authors.initials: L
authors.lastname: Du
authors.affiliation: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University , Jinan, Shandong 250012, China.
authors.forename: Minyong
authors.initials: M
authors.lastname: Li
mesh_terms: D051638:Ether-A-Go-Go Potassium Channels / Q000032:analysis*; D005456:Fluorescent Dyes / Q000032:analysis* / Q000737:chemistry*; D057809:HEK293 Cells; D006801:Humans; D015394:Molecular Structure
chemical_list: D051638:Ether-A-Go-Go Potassium Channels; D005456:Fluorescent Dyes