Issue 80, 2013
From the journal:

Chemical Communications

Bifunctional coumarin derivatives that inhibit transthyretin amyloidogenesis and serve as fluorescent transthyretin folding sensors†

Nojoon Myung,‡a   Stephen Connelly,‡b   Boyoung Kim,‡a   Sung Jean Park,c   Ian A. Wilson,b   Jeffery W. Kellyd  and  Sungwook Choi*a  

* Corresponding authors

a Department of New Drug Discovery and Development, Chungnam National University, Daejon, Republic of Korea
E-mail: swchoi2010@cnu.ac.kr
Fax: +82-42-821-8927
Tel: +82-42-821-8625

b 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

c College of Pharmacy, Gachon University, 534-2 Yeonsu 3-dong, Yeonsu-gu, Incheon 406-799, Republic of Korea

d 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

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.

Graphical abstract: Bifunctional coumarin derivatives that inhibit transthyretin amyloidogenesis and serve as fluorescent transthyretin folding sensors

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Article information

DOI
https://doi.org/10.1039/C3CC44667K
Article type
Communication
Submitted
21 jun 2013
Accepted
06 aug 2013
First published
07 aug 2013

Chem. Commun., 2013,49, 9188-9190

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Bifunctional coumarin derivatives that inhibit transthyretin amyloidogenesis and serve as fluorescent transthyretin folding sensors

N. Myung, S. Connelly, B. Kim, S. J. Park, I. A. Wilson, J. W. Kelly and S. Choi, Chem. Commun., 2013, 49, 9188 DOI: 10.1039/C3CC44667K

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