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等温滴定量热技术在药物研究中的应用 被引量:5

Application of isothermal titration calorimetry in drug research
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摘要 等温滴定量热(ITC)技术是一项可实时、定量、在线和动态描述反应过程的热分析技术,可给出主客体相互作用的结合常数(association constant,KA)、解离常数(disassociation constant,KD)、结合化学计量比(stoichiometry ratio,Δn)、焓变(enthalpychange,ΔH)和熵变(entropychange,ΔS)等热力学参数。该技术具有量热灵敏度高、测量准确等优点。阐述了ITC技术的原理及应用特点,从药物与蛋白之间相互作用、药物与DNA分子间相互作用、临床用药相容性、在药物制剂中的应用及药物与生物膜间相互作用等方面综述了ITC在药物研究领域中的应用进展,并对该技术在非特异性相互作用方面的应用进行了展望。 Isothermal titration calorimetry(ITC) is a real-time, quantitative, on-line, and dynamic thermal analysis technique for describing reaction processes. Some thermodynamic parameters, such as association constant, dissociation constant, stoichiometry ratio, enthalpy change, and entropy change of host and guest interaction, can be obtained in ITC analysis. This technique has the advantages of high calorimetric sensitivity and accurate measurement. In this paper, the principle and application characteristics of ITC technology are described, and the application of this technique in drug research are reviewed, including the interaction between drugs and proteins, the interaction between drugs and DNA molecules, clinical drug compatibility, the application in pharmaceutical preparations and the interaction between drugs and biomembrane. Lastly, the application of this technique in the nonspecific molecular interaction is prospected.
作者 余丹丹 邬瑞光 YU Dan-dan;WU Rui-guang(School of Chinese Materia Medica,Beijing University of Chinese Medicine,Beijing 102488,China)
出处 《中草药》 CAS CSCD 北大核心 2018年第22期5463-5467,共5页 Chinese Traditional and Herbal Drugs
基金 国家自然科学基金资助项目(81773916) 中央高校基本科研业务费专项资金资助(2017-JYB-JS-155)
关键词 等温滴定量热 热分析 特异性相互作用 非特异性相互作用 热力学参数 isothermal titration calorimetry thermal analysis specificity interaction nonspecificity interaction thermodynamic parameters
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