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

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.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Amyloid / antagonists & inhibitors
  • Amyloid / metabolism*
  • Coumarins / chemistry*
  • Escherichia coli / metabolism
  • Humans
  • Prealbumin / antagonists & inhibitors*
  • Prealbumin / metabolism
  • Protein Binding
  • Protein Folding
  • Protein Structure, Quaternary
  • Spectrometry, Fluorescence

Substances

  • Amyloid
  • Coumarins
  • Prealbumin
  • coumarin