Naoko Kotera, Florent Poyer, Anton Granzhan and Marie-Paule Teulade-Fichou
Chem. Commun., 2015,51, 15948-15951
DOI:
10.1039/C5CC06084B,
Communication
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.
