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首页> 外文期刊>Biochemistry >INTERACTIONS OF ACRIDINE ANTITUMOR AGENTS WITH DNA - BINDING ENERGIES AND GROOVE PREFERENCES
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INTERACTIONS OF ACRIDINE ANTITUMOR AGENTS WITH DNA - BINDING ENERGIES AND GROOVE PREFERENCES

机译：CR啶ANT抗原抗体与DNA结合能和凹槽偏好的相互作用。

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Absorbance spectroscopy is used to examine the thermodynamic properties associated with the interaction of the experimental antitumor agents N-[2-(dimethylamino)ethyl]-9-aminoacridine-4-carboxamide (AAC) and N-[2-(dimethylamino)ethyl]acridine-4-carboxamide (DACA) with nucleic acids. Placement of the amino substituent at the C9 position on the acridine ring results in marked changes to the acridine chromophore's electronic properties, with the overall charge of AAC increasing to +2 in comparison to DACA's charge of +1 at neutral pH. In comparative DNA binding studies, we examine the influence that the electrostatic properties of these ligands have on the binding energies as well as their effects on enthalpy and entropy contributions. These studies show that placement of the amino moiety at C9 results in 6 times greater DNA binding affinity as compared the deamino analog (DACA). Comparisons of ionic strength dependence for these two analogs reveal a difference in the binding energies of the compounds which can be attributed to electrostatic effects. Further dissection of the enthalpy and entropy components of the binding energy reveals the enhanced electrostatic effects are related to an increased entropy contribution upon formation of the AAC-DNA complex. Groove selectivity of these acridine analogs was probed by examining the binding profiles to native and groove-modified DNAs which included glycosylated T4 DNA and the distamycin-DNA complex. These studies are indicative of minor groove interactions for both compounds with DNA. [References: 28]
机译：吸收光谱用于检查与实验性抗肿瘤药物N- [2-（二甲基氨基）乙基] -9-氨基ac啶-4-羧酰胺（AAC）和N- [2-（二甲基氨基）乙基]相互作用的热力学性质。 cr啶-4-羧酰胺（DACA）与核酸。将氨基取代基放在the啶环的C9位置会导致marked啶发色团的电子性质发生明显变化，与中性pH时DACA的电荷+1相比，AAC的总电荷增加至+2。在比较性的DNA结合研究中，我们研究了这些配体的静电性质对结合能的影响以及它们对焓和熵贡献的影响。这些研究表明，与脱氨基类似物（DACA）相比，氨基部分在C9处的定位使DNA结合亲和力提高了6倍。对这两个类似物的离子强度依赖性的比较表明，化合物的结合能存在差异，这可以归因于静电效应。结合能的焓和熵成分的进一步剖析表明，增强的静电效应与AAC-DNA复合物形成时熵贡献的增加有关。通过检查与天然和凹槽修饰的DNA（包括糖基化的T4 DNA和双霉素-DNA复合物）的结合情况，可以探究这些a啶类似物的凹槽选择性。这些研究表明两种化合物与DNA的微小沟相互作用。 [参考：28]

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