Published in
Royal Society of Chemistry, Chemical Communications, 88(51), p. 15948-15951, 2015
DOI: 10.1039/c5cc06084b
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Efficient inhibition of human AP endonuclease 1 (APE1) via substrate masking by abasic site-binding macrocyclic ligands
Journal article published in 2015 by
Naoko Kotera,
Florent Poyer,
Anton Granzhan,
Marie-Paule Teulade-Fichou
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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.