title: Bifunctional coumarin derivatives that inhibit transthyretin amyloidogenesis and serve as fluorescent transthyretin folding sensors.
abstract: We describe coumarin derivatives that are non-fluorescent in aqueous buffers and that very selectively bind to transthyretin (TTR) in complex biological environments potently inhibiting TTR amyloidogenesis while also exhibiting sensitive off-on fluorescent sensing of the properly folded quaternary structure of TTR.
authors.affiliation: Department of New Drug Discovery and Development, Chungnam National University, Daejon, 305-764, Republic of Korea.
authors.forename: Nojoon
authors.initials: N
authors.lastname: Myung
authors.affiliation: Department of Integrative Structural and Computational Biology, and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA.
authors.forename: Stephen
authors.initials: S
authors.lastname: Connelly
authors.affiliation: Department of New Drug Discovery and Development, Chungnam National University, Daejon, 305-764, Republic of Korea.
authors.forename: Boyoung
authors.initials: B
authors.lastname: Kim
authors.affiliation: College of Pharmacy, Gachon University, 534-2 Yeonsu 3-dong, Yeonsu-gu, Incheon 406-799, Republic of Korea.
authors.forename: Sung Jean
authors.initials: SJ
authors.lastname: Park
authors.affiliation: Department of Integrative Structural and Computational Biology, and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA.
authors.forename: Ian A
authors.initials: IA
authors.lastname: Wilson
authors.affiliation: Departments of Chemistry and Molecular and Experimental Medicine, and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA.
authors.forename: Jeffery W
authors.initials: JW
authors.lastname: Kelly
authors.affiliation: Department of New Drug Discovery and Development, Chungnam National University, Daejon, 305-764, Republic of Korea.
authors.forename: Sungwook
authors.initials: S
authors.lastname: Choi
mesh_terms: D000682:Amyloid / Q000037:antagonists & inhibitors / Q000378:metabolism*; D003374:Coumarins / Q000737:chemistry*; D004926:Escherichia coli / Q000378:metabolism; D006801:Humans; D011228:Prealbumin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011485:Protein Binding; D017510:Protein Folding; D020836:Protein Structure, Quaternary; D013050:Spectrometry, Fluorescence
chemical_list: D000682:Amyloid; D003374:Coumarins; D011228:Prealbumin; C030123:coumarin