A fluorescent light-up probe as an inhibitor of intracellular β-tryptase

Chem Commun (Camb). 2014 Jun 11;50(46):6120-2. doi: 10.1039/c4cc02208d.

Abstract

A pyrene-functionalized peptidic inhibitor binds to and inhibits β-tryptase in a non-competitive and reversible manner even in cells. Upon protein binding a fluorescence increase of the two pyrene fluorophores is observed which allows using as a fluorescent light-up probe for this enzyme.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Death / drug effects
  • Cell Survival / drug effects
  • Dose-Response Relationship, Drug
  • Fluorescent Dyes / chemical synthesis
  • Fluorescent Dyes / chemistry
  • Fluorescent Dyes / pharmacology*
  • Humans
  • Light*
  • Mast Cells
  • Models, Molecular
  • Molecular Conformation
  • Serine Proteinase Inhibitors / chemical synthesis
  • Serine Proteinase Inhibitors / chemistry
  • Serine Proteinase Inhibitors / pharmacology*
  • Structure-Activity Relationship
  • Tryptases / antagonists & inhibitors*
  • Tryptases / metabolism

Substances

  • Fluorescent Dyes
  • Serine Proteinase Inhibitors
  • Tryptases