Dissemin is shutting down on January 1st, 2025

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Wiley, ChemBioChem, 17(11), p. 2374-2377, 2010

DOI: 10.1002/cbic.201000477

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Bioorthogonal Small Molecule Ligands for PARP1 Imaging in Living Cells

Journal article published in 2010 by Thomas Reiner, Sarah Earley, Anna Turetsky, Ralph Weissleder ORCID
This paper is available in a repository.
This paper is available in a repository.

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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.