Natural product-inspired profluorophores for imaging NQO1 activity in tumour tissues

Bioorg Med Chem. 2019 Sep 1;27(17):3938-3946. doi: 10.1016/j.bmc.2019.07.017. Epub 2019 Jul 15.

Abstract

Herein we designed a collection of trimethyl-lock quinone profluorophores as activity-based probes for imaging NAD(P)H:quinone oxidoreductase (NQO1) in cancer cells and tumour tissues. Profluorophores were prepared via synthetic routes from naturally-occurring quinones and characterised in vitro using recombinant enzymes, to be further validated in cells and fresh frozen canine tumour tissues as potential new tools for cancer detection and imaging.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenocarcinoma / diagnostic imaging*
  • Animals
  • Biological Products / chemical synthesis
  • Biological Products / chemistry*
  • Cell Line
  • Colon / diagnostic imaging
  • Colorectal Neoplasms / diagnostic imaging*
  • Dogs
  • Fluorescent Dyes / chemical synthesis
  • Fluorescent Dyes / chemistry*
  • HL-60 Cells
  • HeLa Cells
  • Humans
  • Kinetics
  • Microscopy, Fluorescence
  • Molecular Structure
  • NAD(P)H Dehydrogenase (Quinone) / analysis
  • NAD(P)H Dehydrogenase (Quinone) / metabolism*
  • Optical Imaging*
  • Quinones / chemical synthesis
  • Quinones / chemistry*

Substances

  • Biological Products
  • Fluorescent Dyes
  • Quinones
  • NAD(P)H Dehydrogenase (Quinone)
  • NQO1 protein, human