Department of Pharmaceutical Chemistry and Drug Analysis, Medical University of Lodz, Muszyńskiego 1, Lodz 90-151, Poland; E-Mails:
Int J Mol Sci. 2012;13(1):427-52. doi: 10.3390/ijms13010427. Epub 2011 Dec 29.
High-throughput screening (HTS) is one of the newest techniques used in drug design and may be applied in biological and chemical sciences. This method, due to utilization of robots, detectors and software that regulate the whole process, enables a series of analyses of chemical compounds to be conducted in a short time and the affinity of biological structures which is often related to toxicity to be defined. Since 2008 we have implemented the automation of this technique and as a consequence, the possibility to examine 100,000 compounds per day. The HTS method is more frequently utilized in conjunction with analytical techniques such as NMR or coupled methods e.g., LC-MS/MS. Series of studies enable the establishment of the rate of affinity for targets or the level of toxicity. Moreover, researches are conducted concerning conjugation of nanoparticles with drugs and the determination of the toxicity of such structures. For these purposes there are frequently used cell lines. Due to the miniaturization of all systems, it is possible to examine the compound's toxicity having only 1-3 mg of this compound. Determination of cytotoxicity in this way leads to a significant decrease in the expenditure and to a reduction in the length of the study.
高通量筛选(HTS)是药物设计中最新的技术之一,可应用于生物和化学科学。这种方法由于利用机器人、探测器和软件来调节整个过程,可以在短时间内对一系列化合物进行分析,并确定与毒性相关的生物结构的亲和力。自 2008 年以来,我们已经实现了该技术的自动化,从而能够每天检查 10 万个化合物。HTS 方法更常与 NMR 或耦合方法等分析技术结合使用,例如 LC-MS/MS。一系列研究使我们能够确定目标的亲和力或毒性水平。此外,还进行了有关将纳米粒子与药物缀合以及确定此类结构的毒性的研究。为此,通常使用细胞系。由于所有系统的小型化,仅使用 1-3 毫克的这种化合物就可以检查化合物的毒性。通过这种方式测定细胞毒性可显著减少支出并缩短研究时间。