Investigating a quadruplex-ligand interaction by unfolding kinetics.

Investigating a quadruplex-ligand interaction by unfolding kinetics.
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DOI:
10.1021/ja0615425
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发表时间:
2006-08-02
影响因子:
15
通讯作者:
Balasubramanian, Shankar
Balasubramanian, Shankar
中科院分区:
化学1区
文献类型:
--
作者:
Green, Jeremy J.;Ladame, Sylvain;Ying, Liming;Klenerman, David;Balasubramanian, Shankar

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我们已经研究了分子内的人端粒DNA G-四链体与半花青肽配体的相互作用,通过研究与互补的DNA寡核苷酸的四链体打开的速率。通过采用最小动力学模型,观察到的四链体开放速率和配体浓度之间的关系,使估计的解离常数。范特霍夫分析显示结合的焓变和熵变分别为−77 ± 22 kJ mol−1和−163 ± 75 J mol−1 K−1。对自由和结合四链体的打开速率常数进行阿克里尼乌斯分析,得到活化能分别为118 ± 2和98 ± 10 kJ mol−1。这些结果表明,配体的存在下,只有一个小的活化能的影响,这表明配体的解结合发生后的过渡态四链体解折叠。
We have investigated the interaction of the intramolecular human telomeric DNA G-quadruplex with a hemicyanine–peptide ligand, by studying the rate of quadruplex opening with a complementary DNA oligonucleotide. By employing a minimal kinetic model, the relationship between the observed rate of quadruplex opening and the ligand concentration has enabled estimation of the dissociation constant. A van't Hoff analysis revealed the enthalpy and entropy changes of binding to be −77 ± 22 kJ mol−1 and −163 ± 75 J mol−1 K−1, respectively. Arrhenius analyses of the rate constants of opening free and bound quadruplex gave activation energies of 118 ± 2 and 98 ± 10 kJ mol−1, respectively. These results indicate that the presence of the ligand has only a small effect on the activation energy, suggesting that the unbinding of the ligand occurs after the transition state for quadruplex unfolding.
DOI: 10.1093/nar/26.5.1167
发表时间: 1998-03-01
影响因子: 14.9
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