具有抑制转甲状腺素蛋白淀粉样变性作用的双功能香豆素衍生物，可作为荧光转甲状腺素蛋白折叠传感器。
Bifunctional coumarin derivatives that inhibit transthyretin amyloidogenesis and serve as fluorescent transthyretin folding sensors.
机构信息
Department of New Drug Discovery and Development, Chungnam National University, Daejon, 305-764, Republic of Korea.
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.
出版信息
Chem Commun (Camb). 2013 Oct 14;49(80):9188-9190. doi: 10.1039/c3cc44667k. Epub 2013 Aug 29.
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.
摘要
我们描述了香豆素衍生物，它们在水性缓冲液中是非荧光的，但在复杂的生物环境中非常选择性地与转甲状腺素蛋白（TTR）结合，强烈抑制 TTR 淀粉样变性，同时还对 TTR 的正确折叠四级结构进行灵敏的开-关荧光感应。
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