title: Design, Synthesis, and Initial Evaluation of Affinity-Based Small-Molecule Probes for Fluorescent Visualization and Specific Detection of Keap1.
abstract: Keap1 is a pluripotent protein which plays a predominant role in cellular homeostasis and stress responses. Given that the cellular environment is quite dynamic and versatile, further investigation of the function of Keap1 depends on tools for specific and real-time detection of Keap1. Herein, we report the development of functional affinity-based small-molecule probes which can overcome some shortcomings of current methods and be applied in further studying the function of Keap1.
authors.affiliation: State Key Laboratory of Natural Medicines and Jiang Su Key Laboratory of Drug Design and Optimization, China Pharmaceutical University , Nanjing 210009, China.
authors.forename: Mengchen
authors.initials: M
authors.lastname: Lu
authors.affiliation: State Key Laboratory of Natural Medicines and Jiang Su Key Laboratory of Drug Design and Optimization, China Pharmaceutical University , Nanjing 210009, China.
authors.forename: Hai-Shan
authors.initials: HS
authors.lastname: Zhou
authors.affiliation: State Key Laboratory of Natural Medicines and Jiang Su Key Laboratory of Drug Design and Optimization, China Pharmaceutical University , Nanjing 210009, China.|Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University , Nanjing 210009, China.
authors.forename: Qi-Dong
authors.initials: QD
authors.lastname: You
authors.affiliation: State Key Laboratory of Natural Medicines and Jiang Su Key Laboratory of Drug Design and Optimization, China Pharmaceutical University , Nanjing 210009, China.|Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University , Nanjing 210009, China.
authors.forename: Zhengyu
authors.initials: Z
authors.lastname: Jiang
mesh_terms: D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D005456:Fluorescent Dyes / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D000072019:Kelch-Like ECH-Associated Protein 1 / Q000032:analysis* / Q000037:antagonists & inhibitors; D015394:Molecular Structure; D054852:Small Molecule Libraries / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D005456:Fluorescent Dyes; C431364:KEAP1 protein, human; D000072019:Kelch-Like ECH-Associated Protein 1; D054852:Small Molecule Libraries