Adaptation of High-Throughput Screening in Drug Discovery—Toxicological Screening Tests

International Journal of Molecular Sciences

Paweł Szymański²  Magdalena Markowicz¹ 

[1] Department of Pharmaceutical Chemistry and Drug Analysis, Medical University of Lodz, Muszyńskiego 1, Lodz 90-151, Poland;

关键词: High-throughput screening (HTS);    cellular microarrays;    drug development;    toxicity;   

DOI  :  10.3390/ijms13010427

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2012 by the authors; licensee Molecular Diversity Preservation International, Basel, Switzerland.