Cyclic perylene diimide: Selective ligand for tetraplex DNA binding over double stranded DNA
Cyclic perylene diimide: Selective ligand for tetraplex DNA binding over double stranded DNA
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环状苝二酰亚胺：四链体 DNA 结合双链 DNA 的选择性配体
DOI：
10.1016/j.bmc.2017.10.014
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发表时间：
2017
影响因子：
3.5
通讯作者：
Shigeori Takenaka
中科院分区：
文献类型：
--
作者：
Suresh Vasimalla;Shinobu Sato;Fuminori Takenaka;Yui Kurose;Shigeori Takenaka
结果表明，在含100 mm KCl50 mM Tris-−缓冲液(pH=7.4Tris- = )中，cPDI的结合常数为6.3 × = 10 6M 1，结合数为n DNA 2与TA核的四链DNA，且对四链DNA的选择性大于双链DNA，达10 3倍以上.圆二色谱表明，在没有K+或Na+离子存在的情况下，加入cPdI后，TA-core诱导了其反平行构象。TRAP法检测PDI抑制端粒酶活性的IC50为0.3 µM，毒副作用低，是一种潜在的抗癌药物。
Synthesized cyclic perylene diimide,cPDI, showed the binding constant of 6.3 × 106M−1with binding number of n = 2 with TA-core as a tetraplex DNA in 50 mM Tris-HCl buffer (pH = 7.4) containing 100 mM KCl using Schatchard analysis and showed a higher preference for tetraplex DNA than for double stranded DNA with over 103times. CD spectra showed that TA-core induced its antiparallel conformation upon addition ofcPDIin the absence or presence of K+or Na+ions. ThecPDIinhibits the telomerase activity with IC50of 0.3 µM using TRAP assay which is potential anti-cancer drug with low side effect.