Bioorthogonal Small-Molecule Ligands for PARP1 Imaging in Living Cells Academic Article uri icon

Overview

MeSH Major

  • Green Fluorescent Proteins
  • Microscopy, Fluorescence
  • Phthalazines
  • Piperazines
  • Poly(ADP-ribose) Polymerases

abstract

  • Crossing borders: Due to recent successes in designing small molecule PARP1 inhibitors, we have synthesized imaging agents for PARP1 based on 1(2H)-phthalazinones. The intracellular distribution of AZD2281-TCO, a transcyclooctene-modified derivative, was visualized by selective reaction with a reactive fluorescent tetrazine. We show that AZD2281-TCO has an IC50 of 11.8 nM, assembles with Tz-fluorophores in the nucleus and colocalizes with PARP1 in live cells. Copyright © 2010 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

publication date

  • November 2010

Research

keywords

  • Academic Article

Identity

Language

  • eng

PubMed Central ID

  • PMC3034378

Digital Object Identifier (DOI)

  • 10.1002/cbic.201000477

PubMed ID

  • 20967817

Additional Document Info

start page

  • 2374

end page

  • 7

volume

  • 11

number

  • 17