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Issue 88, 2015
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Efficient inhibition of human AP endonuclease 1 (APE1) via substrate masking by abasic site-binding macrocyclic ligands

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Abstract

Bis-naphthalene macrocycles, which bind with high affinity and selectivity to abasic sites in DNA, efficiently inhibit their cleavage by APE1 (IC50 = 55–60 nM in the kinetic assay with a model THF substrate). These results demonstrate that substrate masking by non-covalent abasic-site ligands is an efficient strategy for inhibition of APE1.

Graphical abstract: Efficient inhibition of human AP endonuclease 1 (APE1) via substrate masking by abasic site-binding macrocyclic ligands

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Article information


Submitted
21 Jul 2015
Accepted
09 Sep 2015
First published
17 Sep 2015

Chem. Commun., 2015,51, 15948-15951
Article type
Communication

Efficient inhibition of human AP endonuclease 1 (APE1) via substrate masking by abasic site-binding macrocyclic ligands

N. Kotera, F. Poyer, A. Granzhan and M. Teulade-Fichou, Chem. Commun., 2015, 51, 15948
DOI: 10.1039/C5CC06084B

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