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

被引：17

作者：

Kotera, Naoko ^{[1
]}

Poyer, Florent ^{[1
]}

Granzhan, Anton ^{[1
]}

Teulade-Fichou, Marie-Paule ^{[1
]}

机构：

[1] Inst Curie, Ctr Rech, Chem Modelling & Imaging Biol, CNRS,INSERM,U1196,UMR9187, F-91405 Orsay, France

来源：

CHEMICAL COMMUNICATIONS | 2015年 / 51卷 / 88期

关键词：

HUMAN APURINIC/APYRIMIDINIC ENDONUCLEASE-1; BASE-EXCISION-REPAIR; SELECTIVE RECOGNITION; CONTAINING DNA; MOLECULE; METHOXYAMINE; DERIVATIVES; IDENTIFICATION; RESISTANCE; MISMATCH;

D O I：

10.1039/c5cc06084b

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

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.

引用

收藏

页码：15948 / 15951

页数：4

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