Issue 88, 2015

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

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

Supplementary files

Article information

Article type
Communication
Submitted
21 7 2015
Accepted
09 9 2015
First published
17 9 2015

Chem. Commun., 2015,51, 15948-15951

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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