苯并吲哚喹啉与DNA四链体相互作用并抑制端粒酶。

Benzoindoloquinolines interact with DNA tetraplexes and inhibit telomerase.

作者信息

Alberti Patrizia, Schmitt Philippe, Nguyen Chi-Hung, Rivalle Christian, Hoarau Magali, Grierson David S, Mergny Jean-Louis

机构信息

Laboratoire de Biophysique, Muséum National d'Histoire Naturelle, INSERM U 201, CNRS UMR 8646, 43 rue Cuvier, 75231 Paris cedex 05, France.

出版信息

Bioorg Med Chem Lett. 2002 Apr 8;12(7):1071-4. doi: 10.1016/s0960-894x(02)00080-x.

DOI:10.1016/s0960-894x(02)00080-x

PMID:11909720

Abstract

Telomeric G-rich single-stranded DNA can adopt a G-tetraplex structure which has been shown to inhibit telomerase activity. We have examined benzoindoloquinolines derivatives for their ability to stabilize an intramolecular G-quadruplex. The increase in T(m) value of the G-quadruplex was associated with telomerase inhibition in vitro.

摘要

富含鸟嘌呤的端粒单链DNA可形成G-四链体结构，该结构已被证明能抑制端粒酶活性。我们研究了苯并吲哚喹啉衍生物稳定分子内G-四链体的能力。G-四链体的熔解温度（Tm）值升高与体外端粒酶抑制有关。