Bioorthogonal Small-Molecule Ligands for PARP1 Imaging in Living Cells
Green Fluorescent Proteins
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.
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