膜运输蛋白质是不可分的膜蛋白质并且考虑同样潜在的药目标。运输蛋白质的活动试金为开发药指向这些蛋白质是必要的。与对运输蛋白质的活动评价有关的主要问题包括 transporters 和 transporters 的可获得性。研究人员们需要考虑蛋白质的生理的地位(在类脂化合物膜固定或净化) ,底层的可获得性和特性,和活动试金的目的(屏蔽,识别,或比较底层和禁止者) 在选择适当试金策略和技术前。在小囊的膜固定的运输蛋白质能是为借助于举起试金或入口逆流试金越过膜搬运底层的 assayed。或者,运输蛋白质能是为和由使用象等温的滴定热量测定,原子磁性的回声光谱学,或表面电浆子回声那样的技术的 ligands 的相互作用的 assayed。象萤光计,焕发最近试金, electrophysiologi-cal 试金,或站流动试金那样的另外的方法和技术能也被用于运输蛋白质的活动试金。在这份报纸,为对膜运输蛋白质的活动评价的主要策略和技术被考察。
Membrane transport proteins are integral membrane proteins and considered as potential drug targets. Activity assay of transport proteins is essential for developing drugs to target these proteins. Major issues related to activity assessment of transport proteins include availability of transporters, transport activity of transporters, and interactions between ligands and transporters. Researchers need to consider the physiological status of proteins (bound in lipid membranes or purified), availability and specificity of substrates, and the purpose of the activity assay (screening, identifying, or comparing substrates and inhibitors) before choosing appropriate assay strategies and techniques. Transport proteins bound in vesicular membranes can be assayed for transporting substrate across membranes by means of uptake assay or entrance counterflow assay. Alternatively, transport proteins can be assayed for interactions with ligands by using techniques such as isothermal titration calorimetry, nuclear magnetic resonance spectroscopy, or surface plasmon resonance. Other methods and techniques such as fluorometry, scintillation proximity assay, electrophysiological assay, or stopped-flow assay could also be used for activity assay of transport proteins. In this paper the major strategies and techniques for activity assessment of membrane transport proteins are reviewed.