Faculty of Pharmacy, Medical University of Lublin, ul. W. Chodzki 4a, 20-093 Lublin, Poland.
J Pharm Biomed Anal. 2014 Jan;87:313-25. doi: 10.1016/j.jpba.2013.09.003. Epub 2013 Sep 18.
Isothermal titration calorimetry is a versatile method to characterize energetics of intermolecular reactions and in particular interactions between drug molecules and their macromolecular targets. The assay is widely used in medicinal chemistry to quantification and characterization of molecular mechanisms of these interactions. The article reviews applications of the method to study ligand interactions with various classes of embedded membrane proteins. These proteins constitute very important fraction of macromolecular targets for medicinal compounds used in current therapies and recently emerged for detailed structural, functional and biochemical characterization of their interactions with drug molecules.
等温滴定量热法是一种通用的方法,可用于表征分子间反应的热力学性质,特别是药物分子与其大分子靶标之间的相互作用。该测定法在药物化学中广泛用于定量和表征这些相互作用的分子机制。本文综述了该方法在研究配体与各种嵌入膜蛋白的相互作用中的应用。这些蛋白质构成了当前治疗中使用的药物化合物的大分子靶标的重要组成部分,并且最近已经出现了用于详细的结构、功能和生化特性研究其与药物分子的相互作用。