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首页> 外文期刊>Nucleic acids research >Calorimetric and spectroscoptc Investigation of drug - DNA Interactions. I. The binding of netropsin to poly d(AT)
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Calorimetric and spectroscoptc Investigation of drug - DNA Interactions. I. The binding of netropsin to poly d(AT)

机译：量热量和光谱研究药物 - DNA相互作用。 I.北方北方对Poly D（AT）的结合

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We report the first calorlmetric investigation of netropsin binding to poly d(AT). Temperature-dependent uv absorption, circular dichroism (CD), batch calorlmetry, and differential scanning calorimetry (DSC) were used to detect, monitor, and thermodynamically characterize the binding process. The following results have been obtained: 1) Netropsin groove binding is accompanied by a large exothermic enthalpy of 9.2 kcal/mol of drug bound at 25°C. This indicates that a large negative binding enthalpy may be a necessary but not a sufficient criterion for drug intercalation. We suggest that the exothermic binding might be correlated with specific H-bonding interactions. 2) From the difference in DSC transition enthalpies in the presence and absence of netropsin, we calculate a binding enthalpy of ?10.7 kcal/mol of netropsin at 88°C. 3) We calculate a positive AS for netropsin binding to poly d(AT) at 25°C. This positive entropy change may reflect netropsln-induced release of condensed cations and/or bound water. 4) The netropsin-8aturated duplex monophasically melts 46°C higher than the free duplex. The unsaturated duplex melts through two thermally-resolved transitions that correspond to netropsin-free and netropsin-bound regions. These two regions interact dynamically with no substantial influence on the thermal stabilities of the separate domains. 5) Netropsin binding decreases the cooperativity of the duplex to single strand transition.
机译：我们报告了对北方北方北方北方的第一次热量调查（AT）。使用温度依赖性UV吸收，圆形二色（CD），批量压载量和差示扫描量热法（DSC）检测，监测和热力学性地表征结合过程。已经获得以下结果：1）Netropsin沟槽结合伴随着在25℃下的9.2kcal / mol的大量放热焓。这表明大负结合焓可能是必要而不是足够的药物嵌入标准。我们建议放热结合可能与特定的H键合相互作用相关。 2）从DSC过渡焓的差异在存在和不存在的北方，我们在88℃下计算10.7kcal / mol的北方北方的结合焓。 3）我们计算在25℃下与聚d（AT）结合的牛网系数阳性。这种正熵变化可能反映Netropsln诱导的冷凝阳离子和/或结合水的释放。 4）Netropsin-8饱和双相单调，单独熔化46°C高于自由双链体。不饱和双链体通过对应于无北北方的牛腹和北方婚姻区的两种热分辨的转变熔化。这两个地区动态地相互作用，对单独域的热稳定性没有大量影响。 5）Netropsin结合降低了双链体与单链过渡的合作率。

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