当前位置: X-MOL 学术Bioorg. Med. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Cyclic perylene diimide: Selective ligand for tetraplex DNA binding over double stranded DNA
Bioorganic & Medicinal Chemistry ( IF 3.5 ) Pub Date : 2017-10-21 , DOI: 10.1016/j.bmc.2017.10.014
Suresh Vasimalla , Shinobu Sato , Fuminori Takenaka , Yui Kurose , Shigeori Takenaka

Synthesized cyclic perylene diimide, cPDI, showed the binding constant of 6.3 × 106 M−1 with 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 103 times. CD spectra showed that TA-core induced its antiparallel conformation upon addition of cPDI in the absence or presence of K+ or Na+ ions. The cPDI inhibits the telomerase activity with IC50 of 0.3 µM using TRAP assay which is potential anti-cancer drug with low side effect.



中文翻译:

环per二酰亚胺:双链DNA上四链DNA结合的选择性配体

合成的环per二酰亚胺cPDI在含有100 mM KCl的50 mM Tris-HCl缓冲液(pH = 7.4)中显示的结合常数为6.3×10 6  M -1,结合数为n = 2与TA核为四链体DNA使用Schatchard分析,并显示为比双链DNA具有超过10四链DNA更高的优先级3倍。CD光谱显示,在不存在或存在K +或Na +离子的情况下,添加cPDI后TA-core诱导其反平行构象。所述cPDI抑制端粒酶活性与IC 50使用TRAP测定法,其是潜在的抗癌药物副作用低0.3μM的。

更新日期:2017-10-21
down
wechat
bug