Efficient inhibition of human AP endonuclease 1 (APE1) via substrate masking by abasic site-binding macrocyclic ligands?
Chemical Communications Pub Date: 2015-09-17 DOI: 10.1039/C5CC06084B
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.
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Journal Name：Chemical Communications
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CAS no.: 89640-58-4
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